Medicinal Chemistry ResearchThis is an RSS file. You can use it to subscribe to this data in your favourite RSS reader, such as GoogleReader, or to display this data on your own website or blog. Subscribe to this data using MyMedWorm.Subscribe to this data using GoogleReader.Subscribe to this data using Bloglines.Subscribe to this data using MyYahoo.

This page shows you the latest items in this publication.

Pages: 1 2 3 4 5 6 7

314 records returned

Analysis of the essential oil from the aerial parts of Psoralea pubescence (Miq.) Standl and its antibacterial activityEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract The essential oil from aerial parts of Psoralea pubescence (Miq.) Standl (Leguminoseae) was analyzed by gas chromatography (GC) and GC/mass spectroscopy systems. The major components identified were psoralen (24.8%), bakuchiol (21.3%), β-caryophyllene (8.5%), germacrene D (6.8%), and α-humulene (4.6%). The major volatiles released by β-glucosidase treatment of the aqueous plant residue were δ-pinene (28.3%), germacrene D (13.6%), and tricyclene (10.2%). The oil showed significant antibacterial activity against Staphylococcus aureus, Escherichia coli, Klebsiella pneumonia, and Pseudomonas aerugino...
Source: Medicinal Chemistry Research - November 18, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Superoxide anion radical scavenging activity of Cassiasiamea and Cassia javanicaEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This study was designed to explore the antioxidant potential of hexane, chloroform, ethyl acetate, methanol, and water extract of bark and leaves of Cassia siamea and Cassia javanica by superoxide anion radical scavenging assay. The different extracts showed significant inhibition of superoxide radicals in a dose-dependant manner. Among all the bark extracts of C. siamea, the methanol extract showed the maximum inhibition of 60.5% at 800 μg/ml concentration and water extract also showed strong antioxidant potential of 51.3% at 1000 μg/ml concentration. The water extract of bark of C. javanica showed strong a...
Source: Medicinal Chemistry Research - November 13, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Facile and manifest spectrophotometric methods for the determination of six quinolone antibiotics in pharmaceutical formulations using iron saltsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract Simple spectrophotometric methods have been developed for the determination of six quinolone antibiotics, namely, ciprofloxacin, gatifloxacin, norfloxacin, levofloxacin, ofloxacin, and pefloxacin, in pharmaceutical formulations using three different salts of iron. These methods are based on the formation of complexes with ferric nitrate, ferric chloride, or iron ammonium citrate in which the carboxylic group of quinolones undergoes complexation with iron. The complexes formed in these reactions, having a brown color, were measured at their respective λmax values. The increase in absorbance was dire...
Source: Medicinal Chemistry Research - November 11, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Simultaneous determination of pyrimethamine, sulfadoxine, mefloquine, and ibuprofen in pharmaceutical formulations by RP-HPLCEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract A simple and rapid high-performance liquid chromatographic (HPLC) method for simultaneous determination and quantification of pyramethamine, sulfadoxine, mefloquine HCl and ibuprofen was developed. The chromatographic system consisted of a Shimadzu LC-10 AT VP pump, SPD-10 AV VP UV visible detector, and CBM-102 Bus Module integrator. Separation was achieved on a μBondapak 125 A, C-18, 10-μm column at room temperature. The sample was introduced through an injector valve with a 10-μL sample loop. Acetonitrile/water (50:50, v/v) was used as the mobile phase, with a flow rate of 2 mL/min. The pH...
Source: Medicinal Chemistry Research - November 3, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Comparative 3D QSAR study on β1-, β2-, and β3-adrenoceptor agonistsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract A quantitative structure–activity relationship study of tryptamine-based derivatives of β1-, β2-, and β3-adrenoceptor agonists was conducted using comparative molecular field analysis (CoMFA). Correlation coefficients (cross-validated r 2) of 0.578, 0.595, and 0.558 were obtained for the three subtypes, respectively, in three different CoMFA models. All three CoMFA models have different steric and electrostatic contributions, implying different requirements inside the binding cavity. The CoMFA coefficient contour plots of the three models and comparisons among these plots provide clues regardin...
Source: Medicinal Chemistry Research - October 31, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Comparative QSAR modeling of antitumor activity of ARC-111 analogues using stepwise MLR, PLS, and ANN techniquesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract Dibenzo [c,h]-[1,6] naphthyridin-6-one (ARC-111) and its analogues can exhibit potent topoisomerase I targeting and antitumor activities. Quantitative structure-activity relationship (QSAR) studies on the antitumor activity of 22 ARC-111 analogues to RPMI 8402 (expressed as pIC50) were performed by using electronic, spatial, thermodynamic, and topological descriptors based on different chemometric tools including stepwise multiple linear regression (stepwise MLR), partial least squares (PLS), and artificial neural network (ANN). QSAR equations were examined using a training set of 18 compounds and a...
Source: Medicinal Chemistry Research - October 31, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Synthesis and evaluation of a series of aminocyanopyridines as antimicrobial agentsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract With the aim of developing potential antimicrobials, a series of 2-amino-3-cyanopyridines incorporating both sulfur and oxygen as part of the heteroaromatic ring (methyl thiophene, methyl furan) and fused cycloalkane groups were synthesized and characterized by FTIR, 1H-NMR, 13C-NMR, and bases of elemental analysis. All synthesized compounds were evaluated for their in vitro antibacterial and antifungal activity. Antibacterial and antifungal activities of aminocyanopyridines against Pseudomonas aeruginosa ATCC 29212, Bacillus subtilis RSKK 244, Bacillus megaterium (clinical isolate), the gram-positiv...
Source: Medicinal Chemistry Research - October 29, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

QSAR studies of imidazopyridine derivatives as Et-PKG inhibitors using the PSO-SVM approachEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract In this work, the multiple linear regression (MLR) and support vector machine (SVM) methods were applied for modeling and predicting the inhibitory activity of imidazopyridine derivatives with two-dimensional (2D) autocorrelation descriptors calculated from the molecular structure alone for the first time. We define the new objective function as fitness, and it can guide the particle swarm optimization (PSO) method to select important descriptors which are responsible for the inhibitory activity of these compounds. The square of the correlation coefficient (R 2 = 0.897), the square of cor...
Source: Medicinal Chemistry Research - October 29, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Inhibitory effect of Gymnema Montanum leaves on α-glucosidase activity and α-amylase activity and their relationship with polyphenolic contentEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract The present study was attempted to investigate the effect of G. montanum leaf extract on inhibition of α-glucosidase and α-amylase activity. The ethanol extract of G. montanum (GLEt) at various concentrations (1–10 μg/ml) was tested for its inhibition pattern against α-glucosidase and α-amylase activity in vitro and compared with the commercially available α-glucosidase inhibitor, acarbose. The GLEt showed competitive inhibition against yeast α-glucosidase and noncompetitive inhibition against salivary α-amylase in a concentration-dependent manner. Further, we investigated the effect o...
Source: Medicinal Chemistry Research - October 28, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Binding of sodium houttuyfonate analogues to bovine serum albumin revealed by fluoresence quenching studyEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract The binding reaction of sodium houttuyfonate analogues (SHAs) to bovine serum albumin (BSA) was studied by fluorescence quenching. Both dynamic and static interactions are involved in the quenching process. SHAs with shorter carbon chains are more likely to undergo a predominantly dynamic quench over a static quench. In contrast, SHAs with longer carbon chains act as static quenchers. Quench efficiency is in the order SHA-C8 > SHA-C10 > SHA-C12 ≈ SHA-C14 > SHA-C6. It was also observed that the two tryptophan residues of BSA are accessible to SHAs. Mo...
Source: Medicinal Chemistry Research - October 14, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Design, synthesis and preliminary antiviral screening of new N-phenylpyrazole and dihydroisoxazole derivativesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract A new series of N-phenylpyrazoles and dihydroisoxazles was synthesized starting from α,β-unsaturated ketones in basic media using phenyl hydrazine and hydroxylamine HCl, respectively. Antiviral evaluation of the target compounds revealed that the dihydroisoxazole derivatives have promising antiviral activity against hepatitis A virus and herpes simplex virus type 1. Content Type Journal ArticleCategory Original ResearchDOI 10.1007/s00044-009-9248-yAuthors Adel A. Rashad, Zagazig University Department of Medicinal Chemistry, Faculty of Pharmacy 44511 Zagazig EgyptOsama I. El-Sabbagh, Zagazig Uni...
Source: Medicinal Chemistry Research - October 14, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Synthesis and pharmacological evaluation of newer thiazolo [3,2-a] pyrimidines for anti-inflammatory and antinociceptive activityEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract A new series of thiazolo [3,2-a] pyrimidine derivatives was designed and synthesized using 4-fluoroaniline and ethylacetoacetate as starting material. Anti-inflammatory activity was assessed by the rat paw edema method and antinociceptive activity was evaluated by thermal stimulus technique. The compounds 5-(4-chlorophenyl)-2-(4-fluorobenzylidene)-7-methyl-3-oxo-2,3-dihydro-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid (4-fluorophenyl)amide (3l) and 2-(4-chlorobenzylidene)-5-(4-fluorophenyl)-7-methyl-3-oxo-2,3-dihydro-5H-thiazolo[3,2-a]pyrimidine-6-carboxylic acid (4-fluorophenyl)amide (3q) were foun...
Source: Medicinal Chemistry Research - October 14, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Synthesis and cytotoxic activity of genistein derivativesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract A series of genistein derivatives was prepared and tested in vitro against leukocythemia (HL-60), colorectal adenocarcinoma (HT-29), and human gastric adenocarcinoma (SGC-7901) cell lines. Among these derivatives, 4′,5-di-n-octoxy-7-gem-difluoromethylenegenistein, 9f, had the strongest activity against HL-60, HT-29, and SGC-7901 cells. Content Type Journal ArticleCategory Original ResearchDOI 10.1007/s00044-009-9271-zAuthors Xing Zheng, Nanhua University Institute of Pharmacy and Pharmacology Hengyang 421001 People’s Republic of ChinaXu Yao, Nanhua University Institute of Pharmacy and Phar...
Source: Medicinal Chemistry Research - October 14, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Synthesis of 6-(3-substituted-4H-1,2,4-triazol-4-yl)-2-phenylbenzo[d]oxazoles as potential anticonvulsant agentsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract A series of 6-(3-substituted-4H-1,2,4-triazol-4-yl)-2-phenylbenzo[d]oxazoles was synthesized. The anticonvulsant effect and neurotoxicity of the compounds were calculated with maximal electroshock (MES) test, subcutaneous pentylenetetrazole (Sc-PTZ), and rotarod tests in intraperitoneally injected mice. Among the synthesized compounds, compound 2-phenyl-6-(4H-1,2,4-triazol-4-yl)benzo[d]oxazole (3a) could be considered the potentially most useful and safe therapeutic compound, with ED50 = 29.6 mg/kg, TD50 = 285 mg/kg, and PI = 9.7. Its neurotoxicity was the lowes...
Source: Medicinal Chemistry Research - October 14, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Use of structure-based virtual screening in the investigation of novel human sialidase inhibitorsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract Recent studies have determined the molecular mechanisms underlying the pathological alterations of sialic acid or its conjugates in various human disease states, and the sialic acid modifying enzyme sialidase has been adopted as an attractive therapeutic option for diseases like cancer, diabetes, inflammation, and arteriosclerosis. Isoform human sialidase inhibitors are also a good chemical tool for exploring the differential functions of human sialidases. In the current study, structure-based virtual screening was attempted to identify the compounds containing novel structures for human sialidase i...
Source: Medicinal Chemistry Research - October 14, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Synthesis, characterization, antibacterial, antifungal, and immunomodulating activities of gatifloxacin derivativesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract Gatifloxacin is a synthetic broad-spectrum fluorquinolone antibacterial agent with a 3-methylpiperazinyl-side chain at position 7 and a methoxy group at position 8 of the quinolone ring. In the present study different analogues of gatifloxacin were prepared; the piperazinyl ring was chosen as the center of reaction for synthesizing this series of derivatives. The structures of these derivatives were established using spectroscopic techniques such as IR, 1H NMR, and EIMS. In vitro antibacterial and antifungal activities were evaluated by disc diffusion method and these derivatives were compared with ...
Source: Medicinal Chemistry Research - October 14, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Synthesis and biological evaluation of cyclopenten-1-one Mannich base oxovanadium compoundEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract 2-Hydroxy-3-methyl-2-cyclopenten-1-one Mannich base oxovanadium compound (CPD-VO) was synthesized. The human cancer cell lines SMMC-7721 (liver cancer) and SK-OV-3 (ovary cancer) were tested for their viability by MTT in vitro, which showed that CPD-VO exhibited a remarkable activity against the two cell lines, with IC50 values <0.1 8 and <0.23 μg/ml, respectively. And clonogenic assays showed that CPD-VO at 6.250 μg/ml inhibited colony formation of SMMC-7721 cells by 99.10%. Also, CPD-VO suppressed tumor growth of Hep-A-22 (mouse liver cancer) in mice in vivo. Moreover, the intera...
Source: Medicinal Chemistry Research - October 10, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Three-dimensional QSAR and pharmacophore mapping of biphenyl benzoic acid derivatives as selective human β3-adrenergic receptor agonistsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract Molecular modeling studies were performed to develop a predictive common pharmacophore hypothesis (CPH) and use it for alignment in three-dimensional (3D) quantitative structure-activity relationship (QSAR) studies using CoMFA and CoMSIA, with a diverse set of 80 β3-adrenergic receptor (β3-AR) agonists. Using PHASE (Pharmacophore Alignment and Scoring Engine) six-point CPH with one acceptor, one negative charge, one positive charge, and three rings, features were derived for pharmacophore-based alignment of molecules. CPH was selected by correlating the observed and estimated activity for the trai...
Source: Medicinal Chemistry Research - October 10, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Synthesis and cytotoxicity of 1-phenylethanolamine carboxamide derivatives: effects on the cell cycleEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract Seven novel analogues of 1-phenylethanolamine carboxamide derivatives, 3a–3g, related to carboxamides isolated from Isodon excisus were synthesized and evaluated for their cytotoxic and apoptosis-induction properties against murine B16 and leukemia L1210 cell lines. Compounds containing no substitution at the 4′-position (3a–3d) or containing a 4′-amino (3e–3g) group were investigated. Generally, the amino-containing compounds were slightly more active than their unsubstituted congeners. Also, the indole-containing compounds 3c and 3f gave the strongest cytotoxic activity (IC50 = 2...
Source: Medicinal Chemistry Research - October 6, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Antioxidant phenolic compounds and flavonoids of Mitragyna rotundifolia (Roxb.) Kuntze in vitroEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract Different solvent extracts of leaves and bark of Mitragyna rotundifolia (Roxb.) Kuntze were evaluated by DPPH, ABTS, and FRAP assays, respectively, for antioxidant properties. Total phenolic and flavonoid content was determined as pyrocatechol and rutin equivalents, respectively, and correlated with antioxidant activities. More polar solvent extracts (n-butanol and ethyl acetate) had relatively higher antioxidant activity than nonpolar solvent extracts (petroleum ether). The n-butanol extract also exhibited a higher phenolic and flavonoid content than the other solvent extracts did. The DPPH assay w...
Source: Medicinal Chemistry Research - October 6, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Two- and three-dimensional QSAR studies on benzyl amide-ketoacid inhibitors of HIV integrase and their reduced analoguesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract The discovery of clinically relevant inhibitors of HIV-integrase for antiviral therapy has proven to be a challenging task. Ketoacid-derived inhibitors selectively inhibit the strand transfer reaction of HIV-integrase. To elucidate the structural properties required for HIV-integrase inhibitory activity, we present here the results of two- and three-dimensional (2D and 3D) QSAR studies of a series of 24 benzyl amide derivatives. The 2D-QSAR studies were performed using three methods: the multiple linear regression method (MLR), giving r 2 = 0.9340 and q 2 = 0.8471; the partial ...
Source: Medicinal Chemistry Research - October 6, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Analysis of physicochemical properties for drugs from natureEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract The chemical structure of a compound has a direct influence on its physical, chemical, and biological properties. The present study describes data pertaining to calculations and statistical analysis of the physicochemical parameters of drugs obtained directly or indirectly from nature. The study projects various physiochemical parameters required for their druggability. The study reveals that most of these drugs fall close to Lipinski’s rule of five. Among the reported physicochemical parameters, the number of aromatic rings is most interesting. Illustrations regarding the same are reported, along...
Source: Medicinal Chemistry Research - October 6, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Monitoring of 3D breast carcinoma cell culture using proton magnetic resonance imagingEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract We studied two human mammary carcinoma cell lines, MCF-7(NEO-4) HER-2 negative and MCF-7(HER-2) HER-2 positive, in three-dimensional culture. The aim of the study was to determine the glycosaminoglycan (GAG) concentration in breast cancer cell growth ex vivo. We found that GAG concentration produced by both breast cancer cell lines can be measured with high-field magnetic resonance imaging. Content Type Journal ArticleCategory Original ResearchDOI 10.1007/s00044-009-9259-8Authors Dorota Bartusik, Institute for Biodiagnostics (West) National Research Council Canada 3330 Hospital Drive NW Calgary ...
Source: Medicinal Chemistry Research - October 6, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

QSAR analysis of some novel sulfonamides incorporating 1,3,5-triazine derivatives as carbonic anhydrase inhibitorsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract A QSAR study on a series of sulfonamides incorporating 1,3,5-triazine derivatives was performed to explore the physicochemical parameters responsible for their inhibitory activity of carbonic anhydrase I (CA-I) inhibitors. Physicochemical parameters were calculated using WIN CAChe 6.1. Stepwise multiple linear regression analysis was carried out to derive QSAR models, which were further evaluated for statistical significance and predictive power by internal and external validation. The best QSAR model was selected, having a correlation coefficient R = 0.932, a standard error of estimation ...
Source: Medicinal Chemistry Research - October 6, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Synthesis, antimalarial and antibacterial activities of 3-amino acid- and aryl amine-substituted 2-methyl-3H-quinalzolin-4-onesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract A new series of 2-methyl-3H-quinazolinones substituted at the third position with amino acids (2–5) and aryl amine (6, 7) was designed, synthesized, and analyzed by infrared, NMR, and mass spectral analysis. Further, the compounds were screened for their in vivo antimalarial activity using the rodent malaria parasite Plasmodium yoelii (N-67) with the Swiss mice model. The compounds were also tested for their antibacterial activity. Content Type Journal ArticleCategory Original ResearchDOI 10.1007/s00044-009-9245-1Authors Subramania Nainar Meyyanathan, J.S.S. College of Pharmacy Department of Pha...
Source: Medicinal Chemistry Research - October 6, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Comparative molecular similarity indices analysis for predicting the antihyperglycemic activity of thioglitazonesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract The three-dimensional (3D) quantitative structure-activity relationship method, comparative molecular similarity indices analysis (CoMSIA), was applied to a series of thioglitazones (or thiazolidinediones) to derive structure-activity relationships of their antihyperglycemic activity. Evaluation of 39 aligned compounds from the training set served to establish the various models. Predictions were obtained with CoMSIA steric, electrostatic, hydrophobic, and hydrogen bond acceptor and donor fields (q 2 = 0.51, r 2 = 0.942). The developed model was validated by an external test set of 11 compounds, w...
Source: Medicinal Chemistry Research - October 3, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Effect of two strains of Lactobacillus delbruckii subsp. bulgaricus on nitric oxide generation and antioxidant status of rat small intestineEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract In this article we study the effect of diets supplemented with two strains of Lactobacillus delbruckii subsp. bulgaricus (B3 and A13, which produced the highest and lowest amount of exopolysaccharide, respectively) on generation of intestinal nitric oxide (NO) and antioxidant status. The oxidative status in terms of thiobarbituric acid-reactive substances (TBARS) and NO levels in small intestinal tissues were measured. We also determined intestinal nonenzymatic antioxidant levels after supplementation with two strains of L. delbruckii subsp. bulgaricus. In rats, dietary supplementation with both lact...
Source: Medicinal Chemistry Research - October 2, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Synthesis, structure characterization, and biological evaluation of some new 1,2,3-benzotriazole derivativesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract Ten novel benzotriazole compounds were synthesized. Their chemical structures were confirmed by 1H NMR, IR, and elemental analyses, coupled with three selected single-crystal structures (compounds A2, B3, and B5). Their antimycotic and antitumor activities were also investigated. The title compounds showed some antitumor activities, especially in the case of A3 and A4, which showed the most potent activity of propagation inhibition in liver and galactophore cancer cells. Content Type Journal ArticleCategory Original ResearchDOI 10.1007/s00044-009-9243-3Authors Jun Wan, Nanjing University State Key...
Source: Medicinal Chemistry Research - September 30, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Drug interaction studies of gliquidone with fexofenadine, cetirizine, and levocetirizineEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This study thus supports the safe coadministration of gliquidone and H1-receptor blockers as an effective diabetic health management regimen. Content Type Journal ArticleCategory Original ResearchDOI 10.1007/s00044-009-9252-2Authors M. Saeed Arayne, University of Karachi Lab 9, Department of Chemistry Karachi 75270 PakistanNajma Sultana, University of Karachi Research Institute of Pharmaceutical Sciences, Faculty of Pharmacy Karachi 75270 PakistanHina Shamshad, University of Karachi Research Institute of Pharmaceutical Sciences, Faculty of Pharmacy Karachi 75270 PakistanAgha Zeeshan Mirza, University of Karachi Lab 9,...
Source: Medicinal Chemistry Research - September 30, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Controlled release of bovine serum albumin from chitosan membranes in vitroEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract Chitosan membranes loaded with bovine serum albumin (BSA; BSA/chitosan membranes) were prepared by either oven-drying or lyophilization. The encapsulation of BSA was mostly >80%. Controlled release of BSA from the membranes into phosphate-buffered saline (PBS; pH 7.4) was determined with Coomassie brilliant blue at different time periods. The highest cumulative amount of released BSA was 17.30% after 20 days. The optimized chitosan concentration was found to range from 10 to 20 g/l. The most favorable drying temperature for the membrane preparation was 55°C. And membranes made by lyoph...
Source: Medicinal Chemistry Research - September 30, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Effect of side-chain alteration on hormonal activity of nonsteroidal estrogen antagonistsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract Incorporation of novel side-chains in 3,4-diaryl chromans, an established nucleus present in the nonsteroidal estrogen antagonist centchroman, has been carried out. The effect of variation in the nature of the chain on relative binding affinity (RBA) to estrogen receptor, estrogenicity, and antiestrogenicity has been studied. Presence of hydrazide residue on cis- and trans-3,4-diaryl chromans led to relatively higher RBA and estrogenicity as compared with corresponding acids and esters. Content Type Journal ArticleCategory Original ResearchDOI 10.1007/s00044-009-9238-0Authors Sangita, Central Dru...
Source: Medicinal Chemistry Research - September 30, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Ginsenoside Re downregulates ICAM-1 expression, inhibits polymorphonuclear infiltration, and ameliorates ischemia-reperfusion injuryEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In this study, we investigate the effects of ginsenoside Re on the expression of intercellular adhesion molecule-1 (ICAM-1), neutrophil infiltration, and myeloperoxidase (MPO) activity during reperfusion of ischemic tissue. The model of acute ischemia reperfusion was established by ligating the left anterior descending branch of the coronary artery in Wistar rats. After ginsenoside Re administration, expression of ICAM-1 was measured by Western blotting; hematoxylin and eosin was used to analyze myocardial damage and polymorphonuclear leukocyte (PMN) infiltration. The number of PMNs per high-power field was calculated....
Source: Medicinal Chemistry Research - September 30, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

In vitro interaction studies of diltiazem with H2 receptor antagonistsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract Diltiazem is a well-known cardiovascular drug that is used clinically for the treatment of angina pectoris and hypertension. H2-receptor antagonists are used to treat gastroesophageal reflux, gastric and duodenal ulceration. In vitro interaction studies of diltiazem with H2-receptor antagonists (cimetidine, ranitidine, and famotidine) were investigated by using spectrophotometric and RP-HPLC techniques. The availability of diltiazem was found to be influenced considerably in presence of H2-receptor antagonists. The effect of various dissolution mediums, simulating body environments with respect to pH...
Source: Medicinal Chemistry Research - September 25, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Effects of oleic acid on the tissue factor activity, blood lipids, antioxidant and oxidant parameters of streptozotocin induced diabetic rats fed a high-cholesterol dietEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract Ecological studies have suggested an inverse association between monounsaturated fat intake and total mortality, as well as with coronary heart diseases death. Whether the beneficial effects of olive oil on the cardiovascular system are exclusively due to oleic acid remains to be elucidated. The aim of this study was to investigate the effects of oleic acid consumption for three months on lipid profile, oxidant-antioxidant status and tissue factor (TF) activities in streptozotocin (STZ) induced diabetic rats fed a high-cholesterol diet. Forty rats were divided into 5 groups of 8 rats each as control...
Source: Medicinal Chemistry Research - September 25, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Evaluation of wound healing potential of Calotropis gigantea latex studied on excision wounds in experimental ratsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract The present study was aimed at evaluating the wound healing potential of Calotropis gigantea latex on excision wound induced in rats. Topical application of Calotropis gigantea latex extract ointment (10% w/w in petroleum gel) for 14 days significantly improved wound contraction when compared with control group of rats. The levels of hydroxyproline (collagen), hexosamine, uronic acid, DNA, RNA, and protein in the wound matrix revealed the pro-healing effects of Calotropis gigantea latex. The results obtained were comparable to those of nitrofurazone, a standard drug widely used for wound healing....
Source: Medicinal Chemistry Research - September 24, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Non-toxic inhibition of HIV-1 replication with silver–copper nanoparticlesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract Cu and Ag–Cu mixed alloy nanoparticles displayed significant inhibition to HIV-1 replication with limited toxicity to human cells at relatively low concentrations of metal. A previous study (Elechiguerra et al. in J Nanobiotechnol 3:6–16, 2005) suggested a size-specific Ag nanoparticle can be tailored to block or damage the glycoprotein (gp) 120/gp41 spike or, more specifically, the invariant epitope at the gp120 binding site. Two different protocols were employed to test whether nanoparticles block entry of HIV-1, and in both instances the nanoparticles acted at some point other than initial bin...
Source: Medicinal Chemistry Research - September 24, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Quantitative structure–activity relationships study of photocytotoxicity of miscellaneous porphyrins with amino acid and uracil by gene expression programmingEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract Photodynamic therapy (PDT) is a new medical treatment modality for cancer which employs the combination of light and a photosensitizing drug against cancerous tissue. Quantitative structure–activity relationship (QSAR) study of the photocytotoxicity of miscellaneous porphyrins with amino acid and uracil has been performed. A series of molecular descriptors have been calculated in QSAR for these photosensitizers, with selection of variables and construction of nonlinear QSAR models performed simultaneously by gene expression programming (GEP). These selected descriptors encode different aspects of ...
Source: Medicinal Chemistry Research - September 24, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Probing the structure of human glucose transporter 2 and analysis of protein ligand interactionsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract Diabetes is a metabolic disorder that has emerged recently as a major cause of global concern. Regulation of the blood glucose concentration is essential to maintain the homeostasis. GLUT2, a carrier protein, plays an important role in transporting sugar molecules across the membrane. To understand the function of this carrier molecule, knowledge of its three-dimensional structure is of paramount importance. Homology modeling approach was adopted to decipher the three-dimensional structure and features of human GLUT2. Ninety-eight percent residues of the modeled structure lie in the allowed region o...
Source: Medicinal Chemistry Research - September 18, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Quantitative structure–activity relationships for estimating the aryl hydrocarbon receptor binding affinities of resveratrol derivatives and the antioxidant activities of hydroxystilbenesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract Quantitative structure–activity relationships (QSARs) were developed for the aryl hydrocarbon receptor (AhR) binding affinity of non-fluorinated and fluorinated cis and trans 3,4′,5-substituted resveratrol derivatives. Lower quality QSAR fits were found when all compounds were modeled together, in contrast to strong correlations with Hammett substituent constants and atomic charges for separate non-fluorinated/fluorinated and cis/trans groupings. The collective findings suggest little promise in developing new resveratrol derivatives with significantly higher AhR binding affinity beyond the rang...
Source: Medicinal Chemistry Research - September 17, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Removal of vanadium by combining desferrioxamine and deferiprone chelators in ratsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract Investigations were conducted to evaluate the ability of two chelators, desferrioxamine (DFO), and deferiprone (1,2-dimethy1-3-hydroxypyride-4-one, L1), for the excretion of vanadium after a period of administration of vanadium salts in 6-week-old male Wistar rats. Immediately after 60 days of vanadium administration, the rats received chelators (L1, DFO or L1 + DFO) for a period of 1 week. Chelators were given orally (L1), intraperitoneally (DFO), or both to different groups of rats at two different dosage levels. After chelation therapy, animals were sacrificed by exsanguination...
Source: Medicinal Chemistry Research - September 17, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Chemical composition and antimicrobial activity of extracts from Gliocladium sp. growing wild in TunisiaEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract The chemical composition of chloroformic, ethyl acetate, butanolic, and methanolic extracts isolated from the fungus Gliocladium sp. using different solvents of increasing polarity was analyzed by GC-FID and GC-MS. Furthermore, the antimicrobial activity of extracts was tested against five Gram-positive and Gram-negative bacteria and four pathogenic fungi. The tested extracts exhibited an interesting antibacterial activity against all bacteria tested, even against Gram-negative bacteria presenting frequently a higher resistance and against all fungi except Candida albicans. Content Type Journal ...
Source: Medicinal Chemistry Research - August 22, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Synthesis and antimicrobial study of fluoroquinolone-based 4-thiazolidinonesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract The title compounds 2-substituted phenyl-3-{1-cyclopropyl-6-fluoro-7-[4-(4-methoxyphenylpiperazin-1-yl]-4-oxo-1,4-dihydroquinoline} carboxamido-1,3-thiazolidin-4-ones 6a–j have been synthesized from lead molecule 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 1; this reacted with thionyl chloride to give acid chloride 2 and with hydrazine hydrate to afford hydrazide 3. The hydrazide 3 on condensation with substituted aromatic aldehydes a–j gave Schiff base; these on reaction with N-(4-methoxyphenyl) piperazine and thioglycolic acid furnished title compounds 6a–j. All...
Source: Medicinal Chemistry Research - July 29, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Pharmacological characteristics of some 3-salicylidenehydrazono-2-indolinone coordination compoundsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract 3-Salicylidenehydrazono-2-indolinone (SHI) complexes with Co(II), Ni(II), Cu(II), Zn(II), and Pd(II) were synthesized. All compounds were evaluated for their antimicrobial activity against seven pathogenic bacteria and four fungi. The compounds also have been screened for anti-inflammatory activity. The complexes have better antimicrobial and anti-inflammatory than ligand itself. The in vitro antiamoebic activity was evaluated against the HM1:IMSS strain of Entamoeba histolytica, and the results were compared with the standard drug, metronidazole. The preliminary test results showed that the complexe...
Source: Medicinal Chemistry Research - July 29, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Interaction studies of a novel Co(II)-based potential chemotherapeutic agent with human serum albumin (HSA) employing biophysical techniquesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract Novel macrocyclic cobalt(II) complex C36H24N8O4S4CoCl2 with a butterfly topology was synthesized and characterized by spectroscopic (IR, 1H, 13C NMR, EPR, UV-Vis, ESI-MS) and analytical methods. The complex exhibits distorted octahedral geometry around Co(II) metal ion, which was confirmed by EPR measurements with ga, gb, and gc values (8.01, 2.20, and 1.66), respectively, and molar extinction coefficient ε = 58 M−1cm−1. The Interaction studies with human serum albumin (HSA) in phosphate buffer (0.1 M, pH 7.0) were studied by electronic absorption titration, fluorescence titra...
Source: Medicinal Chemistry Research - July 28, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Molecular docking study on anticancer activity of plant-derived natural productsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract A variety of compounds from plant sources have been reported to possess substantial anticancer properties; however, their modes of action have not been clearly defined. Selected plant-derived compounds that exhibit anticancer activity were subjected to docking simulations using AutoDock 3.0.5. To preliminarily investigate the potential molecular targets and to confirm the experimental activity testing for these anticancer compounds, the docking was performed using different enzymes and receptor proteins involved with cell cycle, cell growth, and DNA replication, i.e., cyclin-dependent protein kinase...
Source: Medicinal Chemistry Research - July 28, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Design and synthesis of new 2-aryl, 3-benzyl-(1,3-oxazolidine or 1,3-thiazolidine)-4-ones as selective cyclooxygenase (COX-2) inhibitorsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract A new series of 2-aryl, 3-benzyl-(1,3-oxazolidine or 1,3-thiazolidine)-4-ones, possessing a methylsulfonyl pharmacophore, were synthesized to evaluate their biological activities as selective cyclooxygenase-2 (COX-2) inhibitors. In vitro COX-1 and COX-2 isozyme inhibition studies were performed to acquire structure-activity relationship data with respect to the point that molecular modeling studies showed that designed compounds bind in the primary binding site such that the C-2 para-SO2Me substituent inserts into the 2° pocket present in COX-2 enzyme. COX-1 and COX-2 inhibition studies showed that ...
Source: Medicinal Chemistry Research - July 26, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Synthesis of new pyridazinone derivatives as platelet aggregation inhibitorsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract This paper describes the synthesis and the antiplatelet activity of a series of 6-(4-(substituted-amino)phenyl)-4,5-dihydro-3(2H)-pyridazinones. Antiplatelet activity was determined by using the tail transaction bleeding test. All of the newly synthesized pyridazinone derivatives exhibited significant platelet aggregation inhibitory activity. The compounds IIIc and IIIh displayed two times more platelet aggregation inhibitory effect compared with standard drug aspirin. Content Type Journal ArticleCategory Original ResearchDOI 10.1007/s00044-009-9232-6Authors Sridhar Thota, Panjab University Univer...
Source: Medicinal Chemistry Research - July 25, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Synthesis, chemical characterization of novel 1,3-dimethyl acridones as cytotoxic agents, and their DNA-binding studiesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract A series of new 1,3-dimethyl acridone derivatives were synthesized with different alkyl side chain (propyl and butyl) substitution at N10-position and highly basic amine groups at terminal end of alkyl side chain. All the synthesized molecules were screened for their cytotoxic activity against human breast adenocarcinoma (MCF-7) and human promyelocytic leukemia (HL-60) cell lines. DNA binding constants (Ki) of selected compounds were determined with calf-thymus DNA. Results showed that the molecules 7, 8, 10, 11, 12, 13, 14, and 15 exhibited good cytotoxic activity with IC50 value <10 μM. Co...
Source: Medicinal Chemistry Research - July 6, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

Optimization of microwave-assisted extraction of solanesol from potato leaves and stemsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Abstract Microwave-assisted extraction (MAE) was developed for the fast extraction of solanesol from potato leaves and stems. The ratio of raw material to ethanol, extraction time, extraction temperature, and microwave irradiation power were interdependent. The yield of solanesol reached its maximum 98.57% with 1:8.0 g/ml, 40 min, 55°C, and 2.0 KW, respectively. MAE was comparable to other extraction methods, including solvent extraction, heat-reflux, and Soxhlet-extraction. MAE reduced extraction time, solvent consumption, and increased yields of solanesol. Solanesol concentration was perfor...
Source: Medicinal Chemistry Research - June 23, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals

In vitro drug interaction studies of atorvastatin with ciprofloxacin, gatifloxacin, and ofloxacinEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
We describe the in vitro availability of atorvastatin, a potent HMG-CoA reductase inhibitor, in presence of ciprofloxacin, gatifloxacin, and ofloxacin, all with a wide antibacterial spectrum. These studies were performed at 37°C, 48°C, and 60°C in different pH environments, simulating human body compartments. The reactions were studied by UV spectroscopy, and the availability of both the drugs in presence of each other was determined by deriving a simultaneous equation for two component system through modification of Beer’s law. It has been observed that due to interaction, the availability of both atorvastatin an...
Source: Medicinal Chemistry Research - June 13, 2009 Category: Chemistry Tags: Medicinal Chemistry Research Source Type: journals