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503 records returned

Development of Dinuclear Vanadium Catalysts for Enantioselective Coupling of 2-Naphthols via a Dual Activation Mechanism.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
This review describes our recent efforts in the development of chiral dinuclear vanadium complexes which work as dual activation catalysts for oxidative coupling of 2-naphthols. A chiral dinuclear vanadium(IV) complex (R(a),S,S)-1a possessing (S)-tert-leucine moieties at the 3,3'-positions of the (R)-binaphthyl skeleton was developed, and found to promote oxidative coupling of 2-naphthol to afford (S)-1,1'-bi-2-naphthol (BINOL) with 91% ee. To verify the dual activation mechanism, mononuclear vanadium(IV) complex (S)-10 was also prepared. Kinetic analysis revealed that the reaction rate of oxidative coupling of 2-napht...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Takizawa S Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Oxygenated Cembranoids from the Cultured and Wild-Type Soft Corals Sinularia flexibilis.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Two new cembranoids, flexibilisolide A (1) and flexibilisin A (2), along with one known combranoid 5 have been isolated from the cultured soft coral Sinularia flexibilis. Furthermore, two new cembranoids, flexibilisolide B (3) and flexibilisin B (4), along with two known combranoids (5, 6), have been isolated from the wild-type soft coral S. flexibilis. The structures of the new metabolites were determined on the basis of extensive spectroscopic analysis and by comparison of NMR data with those of known compounds. The metabolites 5 and 6 have been shown to exhibit weak cytotoxic activity against MCF-7 cancer cell line....
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Su JH, Lin YF, Lu Y, Yeh HC, Wang WH, Fan TY, Sheu JH Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Dynamic Influence of the Two Membrane-Proximal Immunoglobulin-Like Domains upon the Peptide-Binding Platform Domain in Class I and Class II Major Histocompatibility Complexes: Normal Mode Analysis.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Major histocompatibility complexes (MHCs) mainly fall into class I and class II. The two classes have similar structures, with two membrane-proximal immunoglobulin-like domains and a peptide-binding platform domain, though their organizations are different. We simulated the dynamics of a whole and partial model deficient in either of the two membrane-proximal domains for class I and class II using normal mode analysis. Our study showed that the influence of the two membrane-proximal domains upon the dynamics of the platform domain were decisively different between class II and class I. Both membrane-proximal domains (t...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Nojima H, Kanou K, Kamiya K, Atsuda K, Umeyama H, Takeda-Shitaka M Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Synthesis and Biological Activity of a New Class of Sulfone-Linked Pyrrolylpyrazoles and Pyrrolylisoxazoles from Methyl-3-aryl-2-(E-arylethenesulfonyl)acrylate.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
A new class of sulfone-linked bis heterocycles, methyl-3-(4'-aryl-1'H-pyrazol-3'-ylsulfonyl)-4-aryl-3H-pyrrole-3-carboxylate (8), methyl-3-(1'-phenyl-3',5'-diaryl-1'H-pyrazol-4'-ylsulfonyl)-4-aryl-3H-pyrrole-3-carboxylate (9) and methyl-3-(3',5'-diarylisoxazol-4'-ylsulfonyl)-4-aryl-3H-pyrrole-3-carboxylate (10) were prepared by the regioselective reaction of methyl-3-aryl-2-(E-arylethenesulfonyl)acrylate (2) with tosylmethyl isocyanide followed by fuctionalization of olefin moiety with 1,3-dipolar reagents. The lead compounds were tested for their antimicrobial activity. PMID: 19881267 [PubMed - in process] (Source...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Padmavathi V, Radha Lakshmi T, Mahesh K, Padmaja A Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Potential Use of 2-Hydroxypropyl-beta-cyclodextrin for Preparation of Orally Disintegrating Tablets Containing dl-alpha-Tocopheryl Acetate, an Oily Drug.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
To expand the application of a drug in orally disintegrating tablets, the potential use of beta-cyclodextrin (beta-CyD) and 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CyD) as excipients for the tablets containing dl-alpha-tocopheryl acetate (VE), an oily drug, was evaluated. HP-beta-CyD, not beta-CyD, solubilized VE in water through the formation of higher order of complexes at the molar ratio of 1 : 2 (VE : HP-beta-CyD). When prepared under the optimal preparation conditions, the VE tablets containing lactose and 5% (w/w) of HP-beta-CyD, not beta-CyD, had high hardness more than 4 kg and rapid disintegration within 10...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Motoyama K, Nagatomo K, Elazim SO, Hirayama F, Uekama K, Arima H Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Formulation and evaluation of press coated tablets for pulsatile drug delivery using hydrophilic and hydrophobic polymers.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
The aim of present investigation was to develop press coated tablet for pulsatile drug delivery of ketoprofen using hydrophilic and hydrophobic polymers. The drug delivery system was designed to deliver the drug at such a time when it could be most needful to patient of rheumatoid arthritis. The press coated tablets containing ketoprofen in the inner core was formulated with an outer shell by different weight ratio of hydrophobic polymer (micronized ethyl cellulose powder) and hydrophilic polymers (glycinemax husk or sodium alginate). The release profile of press coated tablet exhibited a lag time followed by burst rel...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Rane AB, Gattani SG, Kadam VD, Tekade AR Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Synthesis of Ranolazine Metabolites and Their Anti-myocardial Ischemia Activities.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
The anti-anginal drug Ranolazine, a partial fatty acid oxidation (pFOX) inhibitor, is thought to modulate the metabolism during myocardial ischemia by activating pyruvate dehydrogenase activity to promote glucose oxidation. Ranolazine and its five principal metabolites: CVT-2512, CVT-2513, CVT-2514, CVT-2738 and CVT-4786, were synthesized. The effect of Ranolazine and its metabolites on the ECG (electrocardiogram) of mice with myocardial ischemia induced by isoprenaline and their effect on alleviating the symptom of myocardial ischemia were tested and compared. The results showed that CVT-2738 and CVT-2513 could be pro...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Yao Z, Gong S, Guan T, Li Y, Wu X, Sun H Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Reduction-triggered fluorescence probe for Peptide-templated reactions.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
We developed a new nucleic acid-based fluorescence probe for protein detection. The method is based on the scission of an aptamer into two probes, which are then attached with a chemically reactive fluorogenic compound. The protein-dependent association of the two probes accelerates a reduction-triggered fluorogenic reaction and indicates the presence of the target protein, which is detected using a fluorescence readout. The fluorescence signal is generated via the deprotection of the azidomethyl group of fluorescein. The arginine-rich motif peptide of the human immunodeficiency virus-1 Rev protein was targeted by this...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Shibata A, Abe H, Furukawa K, Tsuneda S, Ito Y Tags: Chem Pharm Bull (Tokyo) Source Type: journals

The Constituents and Their Bioactivities of Houttuynia cordata.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Chemical investigation on the whole plant of Houttuynia cordata has resulted in the isolation of two new compounds, named as houttuynoside A (1) and houttuynamide A (2), together with thirty-eight known compounds. The structures of 1 and 2 were elucidated on the basis of spectroscopic analysis. In the inhibitory effects on herpes simplex virus type 1 (HSV-1) assay, norcepharadione B (10) showed good inhibitory activity against the replication of HSV-1. In addition, the antioxidant and antityrosinase activities of some isolated compounds were also evaluated. Among these compounds, quercitrin (25) and quercetin-3-O-beta-...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Chou SC, Su CR, Ku YC, Wu TS Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Stabilization of protein structure in freeze-dried amorphous organic Acid buffer salts.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
The purpose of this study was to elucidate the physical properties and protein-stabilizing effects of some pH-adjusting excipients (carboxylic acids and their sodium salts) in frozen solutions and in freeze-dried solids. Thermal and powder X-ray diffraction (XRD) analysis indicated a high propensity of sodium citrates to form glass-state amorphous solids upon freeze-drying. Some salts (e.g., sodium succinate) crystallized in the single-solute frozen solutions. FT-IR analysis of bovine serum albumin (BSA) and bovine immunoglobulin G (IgG) in the aqueous solutions and the freeze-dried solids showed that some glass-formin...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Izutsu K, Kadoya S, Yomota C, Kawanishi T, Yonemochi E, Terada K Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Analysis of Binding Interaction between Bovine Serum Albumin and the Cobalt(II) Complex with Salicylaldehyde-2-phenylquinoline-4-carboylhydrazone.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
The interaction between bovine serum albumin (BSA) and the cobalt(II) complex with salicylaldehyde-2-phenylquinoline-4-carboylhydrazone (Co-SPC) was investigated using fluorescence spectroscopy, UV absorption, and circular dichroism (CD) under simulated physiologic conditions for the first time. Fluorescence data and UV absorption spectra revealed that the intrinsic fluorescence of BSA was strongly quenched by Co-SPC in terms of a static quenching process at a lower concentration of the complex and a combined quenching process at a higher concentration of the complex. Binding constants and binding sites were evaluated....
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Liu HY, Xu ZH, Liu XH, Xi PX, Zeng ZZ Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Novel System for Decarboxylative Bromination of alpha,beta-Unsaturated Carboxylic Acids with Diacetoxyiodobenzene.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
A simple and mild method for the conversion of varieties of alpha,beta-unsaturated carboxylic acids to the corresponding bromoalkenes using diacetoxyiodobenzene (IBD) in combination with tetraethyl-ammonium bromide (TEAB) at room temperature is discussed. Advantages of this system are short reaction time, easy work up and gave good to excellent yields. PMID: 19881275 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Fursule RA, Patil PO, Shewale BD, Kosalge SB, Deshmukh PK, Patil DA Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Isolation of Acridone Alkaloids and N-[(4-Monoterpenyloxy)phenylethyl]-Substituted Sulfur-Containing Propanamide Derivatives from Glycosmis parva and Their Anti-herpes Simplex Virus Activity.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Six acridone alkaloids including a new glycosparvarine (1), three limonoids, and four N-[(4-monoterpenyloxy)phenylethyl]-substituted sulfur-containing propanamide derivatives including two new species, (+)-S-deoxydihydroglyparvin (10) and (+)-S-deoxytetrahydroglyparvin (11), were isolated from the branches and the leaves of Glycosmis parva CRAIB collected in the east of Thailand. Antiviral activity evaluation of isolates against herpes simplex virus (HSV) type 1 and 2 disclosed that two acridone alkaloids, glycosparvarine (1) and glycofolinine (4), showed moderate inhibitory activities with 50% effective concentration ...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Chansriniyom C, Ruangrungsi N, Lipipun V, Kumamoto T, Ishikawa T Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Effects of Formulation Parameters on Encapsulation Efficiency and Release Behavior of Risperidone Poly(D,L-lactide-co-glycolide) Microsphere.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
A 4-week sustained release risperidone biodegradable poly(D,L-lactide-co-glycolide) (PLGA) microsphere for the therapy of schizophrenia, the effects of formulation parameters on encapsulation efficiency and release behavior were studied. The risperidone PLGA microspheres were prepared by O/W solvent evaporation method and characterized by HPLC, SEM, laser particle size analysis, GC and HPLC-MS. The results indicated that the morphology of the risperidone PLGA microspheres presented a spherical shape with smooth surface, the particle size was distributed from 32 to 92 mum and the drug encapsulation efficiency was influe...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Su Z, Sun F, Shi Y, Jiang C, Meng Q, Teng L, Li Y Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Photochemical cleavage reactions of 8-quinolinyl sulfonates in aqueous solution.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Photochemical cleavage reactions of 8-quinolinyl benzenesulfonate derivatives and related sulfonates in aqueous solutions are reported. The 8-quinolinyl benzenesulfonates undergo photolysis upon photoirradiation at 300-330 nm to give the corresponding 8-quinolinols and benzenesulfonic acids with the production of only negligible amounts of byproducts. The effects of substituent groups of the 8-quinolinyl moiety and the benzene ring on the photolysis reactions were examined. Based on steady-state mechanistic studies using a triplet sensitizer, a triplet quencher, and electron donors, it was suggested that the photolysis...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Kageyama Y, Ohshima R, Sakurama K, Fujiwara Y, Tanimoto Y, Yamada Y, Aoki S Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Structures of New Phenylbutanoids and Nitric Oxide Production Inhibitors from the Rhizomes of Zingiber cassumunar.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
The methanolic (MeOH) extract from the rhizomes of Zingiber cassumunar showed nitric oxide (NO) production inhibitory effects induced by lipopolysaccharide (LPS) in mouse peritoneal macrophages. From the MeOH extract, six new phenylbutanoids, phlains I-VI, were isolated together with 16 known constituents. The structures of new phenylbutanoids were determined on the basis of physicochemical and chemical evidence. In addition, the inhibitory effects of the principal constituents on the NO production were examined. Among them, phlain III (IC(50)=24 muM), (E)-1-(3,4-dimethoxyphenyl)buta-1,3-diene (69 muM), (E)-1-(2,4,5-tr...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Nakamura S, Iwami J, Matsuda H, Wakayama H, Pongpiriyadacha Y, Yoshikawa M Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Design, synthesis and biological evaluation of hydroxy- or methoxy-substituted phenylmethylenethiosemicarbazones as tyrosinase inhibitors.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
A series of hydroxy- or methoxy-substituted phenylmethylenethiosemicarbazones were designed, synthesized and evaluated as mushroom tyrosinase inhibitors. The results demonstrated that most of target compounds had remarkable inhibitory activities on mushroom tyrosinase. Interestingly, compound 2h was found to be the most potent tyrosinase inhibitor with IC(50) value of 0.18 muM. The possible interaction mode between compound 2h and tyrosinase was proposed. In addition, the 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activities of select compounds (IC(50)<10.0 muM) were also investigated. Compounds 2d, 2e,...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Yi W, Cao RH, Chen ZY, Yu L, Ma L, Song HC Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Quantification of the Levels of CYP2D6 mRNA in Peripheral Blood Leukocytes by Reverse Transcriptase Polymerase Chain Reaction HPLC.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
We developed a sensitive high performance liquid chromatography (HPLC) method for determining CYP2D6 mRNA in peripheral blood leukocytes (PBL) by using competitive reverse transcriptase polymerase chain reaction (RT-PCR). The method is specific, reproducible, and sensitive enough to quantify the absolute amount of low and high abundant CYP2D6 mRNA. The native CYP2D6 transcript and the internal standard, a CYP2D6 deletion RNA, were amplified with similar efficiency in RT-PCR. The PCR products were separated as the corresponding peaks in optimized HPLC. The coefficients of variation for competitive RT-PCR and HPLC determ...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Nagano S, Hosono H, Negishi F, Yanagi M, Homma M, Kohda Y, Watanabe M Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Isolation and Identification of a Novel Chlorophenol from a Cell Suspension Culture of Helichrysum aureonitens.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
A novel chlorophenol, 4-chloro-2-(hepta-1,3,5-triyn-1-yl)-phenol (1), was isolated as the major phenolic compound from the cells of Helichrysum aureonitens suspension cultures. Compound 1 has been proposed to be an intermediate in the acetylene biosynthetic pathway of other acetylenic compounds in Helichrysum spp. The ethanol extract of cell suspension cultures and compound 1 were evaluated for their cytotoxicity against monkey kidney Vero (Vero cells) and human prostate epithelial carcinoma (DU145) cell lines, also, the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) against Mycobac...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Ziaratnia SM, Ohyama K, Hussein AA, Muranaka T, Lall N, Kunert KJ, Meyer JJ Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Identification of a Major Polyphenol and Polyphenolic Composition in Leaves of Camellia irrawadiensis.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
The polyphenolic composition of Camellia irrawadiensis, which is a closely related species of Camellia sinensis (cultivated tea), was investigated. The most predominant polyphenol, a kind of ellagitannin, was isolated from leaves of C. irrawadiensis. Its structure was established as 1,2-di-O-galloyl-4,6-O-(S)-hexahydroxydiphenoyl-beta-D-glucose (2) on the basis of spectral and chemical evidence. Moreover, the polyphenols [catechins, strictinin (1), compound 2, theogallin, and gallic acid] and two methylxanthines (theobromine and caffeine) in leaves of C. irrawadiensis were determined by HPLC-Photodiode array detector a...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Yagi K, Goto K, Nanjo F Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Diterpene Esters and Phenolic Compounds from Sapium insigne (ROYLE) BENTH. ex HOOK. fil.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
From the leaves of Sapium insigne (ROYLE) BENTH. ex HOOK. fil., two new phorbol derivatives, such as 16-hydroxyphorbol-16-acetate (4) and 4beta-deoxy-16-hydroxyphorbol-16-acetate (5) along with twelve known phenolic compounds such as 3-O-caffeoyl quinic acid (1), 1-O-galloyl-beta-D-glucose (2), 1,3-di-O-galloyl-beta-D-glucose (3), rutin (6), 1,3,4,6-tetra-O-galloyl-beta-D-glucose (7), quercetin (8), guaijaverin (9), nicotiflorin (10), scopolin (11), methyl gallate (12), corilagin (13) and 1,3,6-tri-O-galloyl-beta-D-glucose (14) were isolated. All of these compounds have been isolated for the first time from this plant....
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Devkota HP, Basnet P, Yahara S Tags: Chem Pharm Bull (Tokyo) Source Type: journals

A New Amide, Piperchabamide F, and Two New Phenylpropanoid Glycosides, Piperchabaosides A and B, from the Fruit of Piper chaba.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
A new amide, piperchabamide F (1), and two new phenylpropanoid glycosides, piperchabaosides A (2) and B (3), were isolated from 80% aqueous acetone extract from fruit of Piper chaba. Their stereostructures were elucidated on the basis of chemical and physicochemical evidence. PMID: 19881285 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Morikawa T, Yamaguchi I, Matsuda H, Yoshikawa M Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Polycyclic N-Heterocyclic Compounds. Part 60: Reactions of 3-(2-Cyanophenyl)quinazolin-4(3H)-ones with Primary Amines.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
The reaction of 3-(2-cyanophenyl)quinazolin-4(3H)-one with various primary alkylamines gave 3-alkylquinazolin-4(3H)-ones via an addition of the nucleophile, ring opening, and ring closure (ANRORC) mechanism. This type of reaction required hydroxy group functionality in either the solvent or reagent. When hydroxylamine was used as nitrogen nucleophile, the intermediate of this reaction was isolated and found to be an amide oxime. When ethylenediamine was used as the nucleophile, the amidine moiety of the intermediate decomposed to give a benzanilide. PMID: 19881286 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Okuda K, Tagata T, Kashino S, Hirota T, Sasaki K Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Expedient synthesis of mequitazine an antihistaminic drug by palladium catalyzed allylic alkylation of sodium phenothiazinate.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
A short and straightforward synthesis of the antihistaminic drug mequitazine is reported, based on an efficient palladium catalyzed allylic alkylation of 1-aza-bicyclo[2.2.2]oct-2-en-3-ylmethyl acetate using sodium phenothiazinate in mild conditions. PMID: 19881287 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Gonnot V, Nicolas M, Mioskowski C, Baati R Tags: Chem Pharm Bull (Tokyo) Source Type: journals

24-Ethyl,24-methyl-29-nor-lanostanes from Leaves of Freycinetia formosana.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Two new 24-ethyl,24-methyl-29-nor-lanostanes (1, 2) were isolated from the MeOH extract of leaves of Freycinetia formosana (Pandanaceae). Their structures were elucidated based on spectroscopic evidence. PMID: 19881288 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Inada A, Morimoto C, Yoshikawa T, Inatomi Y, Murata H Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Sequence Fourier Analysis of a Specific Protein-DNA (RNA) Interaction; an Intermolecular Frequency Symmetry.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Here, we first report that a specific protein-DNA (RNA) interaction between p53 protein and divergent I kappa B kinase interacting protein (IKIP)-Apaf1 DNA promoter region, and between poliovirus 3CD protein and the 5' terminal region of the RNA sequence can be successfully elucidated with a sequence Fourier analysis, alike various specific protein-protein interactions described previously. Based on these, the intermolecular frequency symmetry would be evolutionarily conserved in a specific interaction of the bioactive structure of various long-chain sequences. In addition, the symmetry is fairly sensitive to a substit...
Source: Chemical and Pharmaceutical Bulletin - November 1, 2009 Category: Drugs & Pharmacology Authors: Numao N, Kamimoto Y Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Development of positron-emission tomography/single-photon emission computed tomography imaging probes for in vivo detection of beta-amyloid plaques in Alzheimer's brains.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Currently, the development of radiotracers for in vivo imaging of beta-amyloid plaques in Alzheimer's disease (AD) brains is an important, active area of molecular imaging. Postmortem brains of AD patients reveal neuropathologic features: the presence of beta-amyloid plaques and neurofibrillary tangles, which contain beta-amyloid peptides and highly phosphorylated tau proteins. Increases in the concentration of beta-amyloid in the course of the disease lead to changes in AD brains. Thus, when used in combination with positron-emission tomography/single-photon emission computed tomography (PET/SPECT), beta-amyloid imagi...
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Ono M Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Improvement of dissolution property of poorly water-soluble drug by supercritical freeze granulation.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
The dissolution property of the poorly water-soluble drug, flurbiprofen (FP) was improved by a novel supercritical freeze granulation using supercritical carbon dioxide. Supercritical freeze granulation was defined as a production method of the granulated substances by using the dry ice to generate intentionally for the rapid atomization of the supercritical carbon dioxide to the atmospheric pressure. This process utilized a rapid expansion of supercritical solutions (RESS) process with the mixture of the drug and lactose. In the supercritical freeze granulation, needle-like FP fine particles were obtained which adhere...
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Sonoda R, Hara Y, Iwasaki T, Watano S Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Anchoring of ulex europaeus agglutinin to chitosan nanoparticles-in-microparticles and their in vitro binding activity to bovine submaxillary gland mucin.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Focused on the natural biodegradable material of chitosan (CS), this investigation concerned its spray-dried nanoparticles-in-microparticles (NiMPs) modified with ulex europaeus agglutinin (UEA). Chitosan nanoparticles were obtained by ionotropic gelation process with pentasodium tripolyphosphate as gelatinizer. Then UEA lectin was bound onto the CS nanoparticles activated by glutaraldehyde. The conjugated spherical UEA-CS-NiMPs, prepared by spray drying method, exhibited 12-85% coupling efficiency of UEA depending upon the amount of activator glutaraldehyde. And the UEA-grafted particles showed additional higher bindi...
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Li FQ, Fei YB, Chen X, Qin XJ, Liu JY, Zhu QG, Hu JH Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Nanoparticulation of poorly water soluble drugs using a wet-mill process and physicochemical properties of the nanopowders.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
In order to improve the dissolution and oral absorption properties of poorly water soluble drugs such as omeprazole, albendazole and danazol, various dispersing agents were added to prepare nanopowder formulations using an ULTRA APEX MILL, which is a wet-mill instrument, and their physicochemical properties were evaluated. Using Pluronic F-108 or F-68 as dispersing agents, slurries containing drug particles having nanometer size were obtained for all model drugs tested. Omeprazole, a heat labile drug, was not degraded by wet-milling and the omeprazole nanoparticles in a milled slurry did not aggregate for 24 h after we...
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Tanaka Y, Inkyo M, Yumoto R, Nagai J, Takano M, Nagata S Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Preparation and evaluation of medicinal carbon tablets with different saccharides as binders.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Medicinal carbon (MC) tablets were prepared with several saccharides to improve the formability and absorption ability of MC tablets made with maltitol (MT). The MC tablets were made by the wet granule compression method, in which maltitol, xylitol (XYL), mannitol (MAN), and sorbitol (SOR) were used as binders. Granule and tablet formability, tablet strength, disintegration, and MC adsorption potential were evaluated for each formulation. Acetaminophen (AA) was used in checking effect of binders on adsorption. Due to low water solubility, MAN was added only up to 30% (w/w) of MC; in greater concentrations, the tablet c...
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Yamamoto K, Ito A, Machida Y Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Nanosizing of poorly water soluble compounds using rotation/revolution mixer.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
In this study, nanoparticles of various poorly water soluble compounds were prepared by wet milling that was carried out using a rotation/revolution mixer and zirconia balls. To be compared with Beads mill, rotation/revolution mixer has superior in very quick process (5 min) and needs very few amounts of zirconia balls (2.4 g) for pulverizing drugs to nanometer range. Phenytoin, indomethacin, nifedipine, danazol, and naproxen were selected as the standard poorly water soluble compounds. Various parameters of the rotation/revolution mixer were studied to decide the optimal pulverization conditions for the production of nano...
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Takatsuka T, Endo T, Jianguo Y, Yuminoki K, Hashimoto N Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Stomach-site specific drug delivery system of clarithromycin for eradication of Helicobacter pylori.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Gellan gum based floating beads containing clarithromycin (FBC) were prepared by iontotropic gelation method for stomach-specific drug delivery against Helicobacter pylori. The scanning electron microscope photograph indicated that prepared beads were spherical in shape with rough outer surface. Formulation variables such as concentrations of gellan, calcium carbonate and drug loading influenced the in vitro drug release characteristics of prepared beads. In vitro release rate of clarithromycin was corrected using first order degradation rate constant which is degraded significantly during the release study in simulate...
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Rajinikanth PS, Mishra B Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Anti-human immunodeficiency virus-1 protease activity of new lanostane-type triterpenoids from Ganoderma sinense.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Five new highly oxygenated lanostane-type triterpenoids [ganoderic acid GS-1 (1), ganoderic acid GS-2 (2), ganoderic acid GS-3 (3), 20(21)-dehydrolucidenic acid N (4) and 20-hydroxylucidenic acid A (5)] were isolated from the fruiting body of Ganoderma sinense, together with known compounds including 6 triterpenoids and 3 sterols. The structures of the new triterpenoids determined by spectroscopic means including 2D NMR were 7beta-hydroxy-3,11,15-trioxo-lanosta-8,24(E)-dien-26-oic acid (1), 7beta,15alpha-dihydroxy-3,11-dioxo-lanosta-8,24(E)-dien-26-oic acid (2), 12beta-acetoxy-3beta,7beta-dihydroxy-11,15-dioxo-lanosta-...
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Sato N, Zhang Q, Ma CM, Hattori M Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Syntheses of glycoclusters containing a phosphocholine residue related to a glycosphingolipid from the earthworm Pheretima hilgendorfi.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Three types of glycoclusters related to an amphoteric glycosphingolipid found in the earthworm Pheretima hilgendorfi were synthesized. The glycoclusters were prepared from a common precursor and a simple approach for the rational design of a glycocluster was developed. PMID: 19801862 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Hada N, Shida Y, Negishi N, Schweizer F, Takeda T Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Structures of new flavonoids and benzofuran-type stilbene and degranulation inhibitors of rat basophilic leukemia cells from the Brazilian herbal medicine Cissus sicyoides.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Three new flavonoid glycosides (cissosides I, II, and III) and a new benzofuran-type stilbene (cissusin) were isolated from the methanolic extract of the aerial parts of Cissus sicyoides cultivated in Brazil. Their structures were elucidated on the basis of chemical and physicochemical evidence. The inhibitory effects of the isolated constituents on the release of beta-hexosaminidase as a marker of degranulation in rat basophilic leukemia (RBL-2H3) cells were examined. Cissusin, flavonols (kaempferol, quercetin), flavones (7,3',4'-trihydroxyflavone, lanceolatin B), pterocarpanes (homopterocarpin), chalcones (isoliquiri...
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Xu F, Matsuda H, Hata H, Sugawara K, Nakamura S, Yoshikawa M Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Generation of formaldehyde by pharmaceutical excipients and its absorption by meglumine.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Formaldehyde is a well-known air impurity. The possibility was investigated in this study that pharmaceutical excipients commonly used in oral solid dosage forms might also be sources of formaldehyde. The results showed that formaldehyde is generated by the excipients lactose, D-mannitol, microcrystalline cellulose, low-substituted hydroxypropylcellulose, magnesium stearate and light anhydrous silicic acid. Since the quality and safety of pharmaceutical products can be significantly affected by the presence of formaldehyde, various amines were then investigated for their ability to decrease levels of formaldehyde using...
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Fujita M, Ueda T, Handa T Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Lactone derivatives from the marine-derived fungus Penicillium sp. PSU-F44.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Two new fungal metabolites, penicipyrone (1), and penicilactone (2), were isolated from the marine-derived fungus Penicillium sp. PSU-F44 along with three known macrolides, (+)-brefeldin A (3), (+)-brefeldin C (4), and 7-oxobrefeldin A (5). Their antimicrobial activities against methicillin-resistant Staphylococcus aureus SK1 and Microsporum gypseum SH-MU-4 were examined. PMID: 19801865 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Trisuwan K, Rukachaisirikul V, Sukpondma Y, Phongpaichit S, Preedanon S, Sakayaroj J Tags: Chem Pharm Bull (Tokyo) Source Type: journals

First syntheses of (-)-tauranin and antibiotic (-)-BE-40644 based on lipase-catalyzed optical resolution of albicanol.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
First syntheses of sesquiterpene quinones (-)-tauranin and (-)-BE-40644 which exhibited strong cytotoxicity against several cancer cell lines, were achieved from (8aS)-albicanol obtained by enzymatic optical resolution. By comparison of the sign of specific rotation between synthetic (12bS)-BE-40644 and natural (-)-BE-40644, the absolute configurations of natural (-)-BE-40644 were determined to be 4aS, 6aS, 12aR, 12bS. PMID: 19801866 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Ishii S, Fujii M, Akita H Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Extended X-ray absorption fine structure study on reaction of anti-tumor platinum complexes with reduced glutathione.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Reactions of cis-diamminedichloroplatinum(II) (cisplatin) and 1,1-cyclobutanedicarboxylatodiammineplatinum(II) (carboplatin) with reduced glutathione, a tripeptide that is abundant in cells, were studied by means of X-ray absorption spectroscopy. Back-scattering amplitudes F(i)(k) and phase shifts Phi(i)(k) were theoretically derived, and validated by applying them to calculate extended X-ray absorption fine structure (EXAFS) oscillations of cisplatin and K(2)[Pt(SCN)(4)] in the solid state. EXAFS oscillations of reaction mixtures of cisplatin or carboplatin with reduced glutathione were fitted to the standard EXAFS eq...
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Obata M, Harada M, Ohi H, Hirohara S, Gottchaldt M, Yano S Tags: Chem Pharm Bull (Tokyo) Source Type: journals

N-glycosides of amino acid amides from Hemerocallis fulva var. sempervirens.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
As part of our search for sedative substances from natural sources, we isolated two novel amino acid amides connected with the fructopyranose, kwansonine A (1) and kwansonine B (2), together with three known amino acid amides, longitubanine A (3), longitubanine B (4), and pinnatanine (5), from Hemerocallis fulva L. var. sempervirens (ARAKI) M. HOTTA. The structures of 1 and 2 have been determined on the spectroscopic evidences as N(2)-(1-beta-D-fructopyranosyl)-N(5)-(2',5'-dihydro-2'-furyl-3'-hydroxymethyl)-gamma-hydroxyglutamine and N(2)-(1-beta-D-fructopyranosyl)-N(5)-(2-hydroxymethylbutadienyl)-gamma-hydroxyglutamin...
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Ogawa Y, Konishi T Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Two new antimicrobial dimeric compounds: febrifuquinone, a vismione-anthraquinone coupled pigment and adamabianthrone, from two Psorospermum species.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Febrifuquinone (1), a new vismione-anthraquinone coupled pigment and a new bianthrone named adamabianthrone (2), were isolated respectively, from the roots of Psorospermum febrifugum and from the bark of Psorospermum adamauense along with eight known compounds including: two bianthrones [(bianthrone A(1) (3) and bianthrone A(2b)], one vismione [(vismione D (4)], one anthrone (3-geranyloxyemodin anthrone) and four anthraquinones [(1,8-dihydroxy-3-isoprenyloxy-6-methylanthraquinone, emodin (5), 3-geranyloxy-1,8-dihydroxy-6-methylanthraquinone and 2-geranyl-1,8-dihydroxy-6-methylanthraquinone]. Their structures were deter...
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Tsaffack M, Nguemeving JR, Kuete V, Ndejouong Tchize Ble S, Mkounga P, Penlap Beng V, Hultin PG, Tsamo E, Nkengfack AE Tags: Chem Pharm Bull (Tokyo) Source Type: journals

New friedelane triterpenoids with antimicrobial activity from the stems of Drypetes paxii.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Two new friedelane-type triterpenes named 12alpha-hydroxyfriedelane-3,15-dione and 3beta-hydroxyfriedelan-25-al, together with six known compounds were isolated from the stems of Drypetes paxii Hutch. (Euphorbiaceae). Their structures were established on the basis of conventional 1 dimensional (1D) NMR methods, 2D shift-correlated NMR experiments and mass spectra. The five friedelane-type triterpene derivatives and one olean-12-ene triterpene saponin were tested for antimicrobial activity against some gram-positive and gram-negative bacteria, and they appeared to be modestly active. PMID: 19801870 [PubMed - in proc...
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Chiozem DD, Trinh-Van-Dufat H, Wansi JD, Mbazoa Djama C, Fannang VS, Seguin E, Tillequin F, Wandji J Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Two new sesquiterpene glucosides from Dennstaedtia scabra (Wall.) Moore.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Two new sesquiterpene glucosides onitioside A (1) and dennstoside B (2), were isolated from the 95% EtOH extract of Dennstaedtia scabra (Wall.) Moore, together with seven known compounds, onitisin (3), pterosin A (4), pinocembrin (5), pinocembrin 7-rutinoside (6), kaempferol (7), nicotiflorin (8), and galangin (9). Their structures were determined by extensive spectroscopic analysis. PMID: 19801871 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Li MM, Wang K, Pan ZH, Chen XQ, Peng LY, Li Y, Cheng X, Zhao QS Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Chantriolide C, a new withanolide glucoside and a new spirostanol saponin from the rhizomes of Tacca chantrieri.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
A new withanolide, chantriolide C (1) and a new spirostanol saponin, chantrieroside A (2) were isolated from the rhizomes of Tacca chantrieri, together with another five known steroidal compounds. Their structures were established as (22R)-1alpha,12alpha-diacetoxy-2alpha,3alpha;6alpha,7alpha-diepoxy-27-[(beta-D-glucopyranosyl)oxy]-5alpha-hydroxywith-24-enolide (1) and (25R)-spirost-5-en-3-yl-O-alpha-L-rhamnopyranosyl-(1-->2)-O-[O-beta-D-glucopyranosyl-(1-->4)-alpha-L-rhamnopyranosyl-(1-->3)]-beta-D-glucopyranoside (2). The structures of the new saponins were determined by detailed analysis of their 1 dimension...
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Zhang L, Liu JY, Xu LZ, Yang SL Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Four new lignans from Viburnum foetidum var. foedidum.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
The 70% aqueous acetone extract of the aerial part of Viburnum foetidum var. foedidum afforded four new lignans (1-4) together with six known ones. The structures of the four new compounds were elucidated on the basis of 1D (dimensional), 2D-NMR, and mass spectral analysis. The structure of compound 1, with a novel spirocyclic moiety, was also confirmed by X-ray diffraction analysis. Compounds 1-10 were evaluated for their cytotoxic activity. However, none of the compounds showed significant cytotoxic activity. PMID: 19801873 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Chen XQ, Li Y, He J, Wang K, Li MM, Pan ZH, Peng LY, Cheng X, Zhao QS Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Three new diterpenoids from the fruit of Vitex agnus-castus.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
Three new labdane-type diterpenoids, viteagnusins F, G, and H, were isolated from the hexane extract of fruit (chasteberry) of Vitex agnus-castus L. (Verbenaceae) along with seven known compounds including four labdane-type diterpenoids, one norlabdane-type diterpenoid, one aromadendrane-type sesquiterpenoid, and one flavonoid. The chemical structures of the three new labdane-type diterpenoids were determined on the basis of spectroscopic data as well as chemical evidence. PMID: 19801874 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Ono M, Nagasawa Y, Ikeda T, Tsuchihashi R, Okawa M, Kinjo J, Yoshimitsu H, Nohara T Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Haliclonacyclamines, tetracyclic alkylpiperidine alkaloids, as anti-dormant mycobacterial substances from a marine sponge of Haliclona sp.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
A new tetracyclic alkylpiperidine alkaloid, 22-hydroxyhaliclonacyclamine B (1), together with two known alkaloids, haliclonacyclamine A (2) and B (3), were isolated from a marine sponge of Haliclona sp. as anti-dormant mycobacterial substances. The chemical structure of 22-hydroxyhaliclonacyclamine B (1) was determined on the basis of spectroscopic study. The compounds 2 and 3 showed strong anti-mycobacterial activity against Mycobacterium smegmatis and M. bovis Bacille de Calmette et Guérin (BCG) under both aerobic condition and hypoxic condition inducing dormant state with minimum inhibitory concentrations (MICs...
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Arai M, Ishida S, Setiawan A, Kobayashi M Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Isolation, synthesis, and bioactivity of homoisoflavonoids from Caesalpinia pulcherrima.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
One new homoisoflavonoid, (3E)-2,3-dihydro-6,7-dimethoxy-3[(3-hydroxy-4-methoxyphenyl)methylene]-4H-1-benzopyran-4-one and four naturally new analogues, (3E)-3-(1,3-benzodioxol-5-ylmethylene)-2,3-dihydro-7-hydroxy-4H-1-benzopyran-4-one, (3E)-3-(1,3-benzodioxol-5-ylmethylene)-2,3-dihydro-7-methoxy-4H-1-benzopyran-4-one, (3E)-2,3-dihydro-7-hydroxy-3-[(3-hydroxy-4-methoxyphenyl)methylene]-4H-1-benzopyran-4-one and (3E)-2,3-dihydro-3-[(3,4-dimethoxyphenyl)methylene]-7-methoxy-4H-1-benzopyran-4-one, along with four known homoisoflavonoids, bonducellin, sappanone A, 2'-methoxybonducellin and 7-O-methylbonducellin were isolat...
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Das B, Thirupathi P, Ravikanth B, Aravind Kumar R, Sarma AV, Basha SJ Tags: Chem Pharm Bull (Tokyo) Source Type: journals

Synthesis and reaction of 1-azabicyclo[3.1.0]hexane.email this articleEmail this article to a colleague. save this article to My ClippingsSave this article to My Clippings. discuss this articleDiscuss or comment on this article.
The effective formation of 1-azabicyclo[3.1.0]hexane (5) by treatment of 2-(bromomethyl)pyrrolidine hydrobromide (4) with n-BuLi was established, with the reaction occurring by a rational reaction pathway via the open chain transition state 8 based on intermolecular Br...Li(+) coordination (SN2 process). The reaction of 5 with electrophiles 13a-n gave the corresponding pyrrolidines 14a-n and piperidine 6, 15a-g, i-n. The selectivity of the products in this reaction appeared to be controlled by equilibrium. PMID: 19801877 [PubMed - in process] (Source: Chemical and Pharmaceutical Bulletin)
Source: Chemical and Pharmaceutical Bulletin - September 30, 2009 Category: Drugs & Pharmacology Authors: Hayashi K, Kujime E, Katayama H, Sano S, Shiro M, Nagao Y Tags: Chem Pharm Bull (Tokyo) Source Type: journals