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191 records returned

Synthesis and Antistaphylococcal Activity of N-Substituted-1H-benzimidazole-sulphonamidesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
A series of N-substituted-1H-benzimidazole-5(6)-sulfonamides and 3-(5,6-dichloro-1H-benzimidazol-2-yl)-N-substituted benzensulfonamides were synthesized and evaluated for antibacterial activity against Staphylococcus aureus and methicillin-resistant S. aureus (MRSA). Certain compounds inhibit bacterial growth with low MIC ([mu]g/mL) values. The most active compounds 30, 31, and 32 have the lowest MIC values with 0.39 to 0.19 [mu]g/mL. Among the compounds having sulfonamido moities, 16, 23, and 24 exhibited the strongest antibacterial activity with 1.56 [mu]g/mL MIC values. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - November 20, 2009 Category: Drugs & Pharmacology Authors: M. Orhan Püsküllü, Sulhiye Y[inodot]ld[inodot]z, Hakan Göker Source Type: journals

Synthesis and Antiproliferative Activitiy of Novel Diaryl Ureas Possessing a 4H-Pyrido[1,2-a]pyrimidin-4-one GroupEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
We herein disclose a series of novel diaryl urea derivatives possessing a 4H-pyrido[1,2-a]pyrimidin-4-one group as novel potent anticancer compounds. The structures were confirmed by IR, 1H-NMR, and MS. All the compounds were screened for their antiprofilerative activity agaist the human breast cancer cell line (MDA-MB-231). The pharmacological results indicated that most of the compounds showed moderate activity. The best of this series is compound 4c (IC50 = 0.7 [mu]mol/L), with a potency 3.6-fold higher than Sorafenib (IC50 = 2.5 [mu]mol/L), which was approved in 2005. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - November 19, 2009 Category: Drugs & Pharmacology Authors: Peng Yao, Xin Zhai, Dong Liu, Bao Hui Qi, Hai Liang Tan, Yong Cai Jin, Ping Gong Source Type: journals

Fungicide Activity of 5-(4-Chlorobenzylidene)-(Z)-2-dimethylamino-1,3-thiazol-4-one against Cryptococcus NeoformansEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The present work describes the synthesis and antifungal evaluation of new 5-arylidene-(Z)-2-dimethylamino-1,3-thiazol-4-ones 4a-f, obtained by the reaction of aromatic aldehydes 1 and rhodanine 2 followed by treatment with DMF. All compounds were tested against a panel of yeasts, hialohyphomycetes, and dermatophytes using the microbroth dilution method. Compounds 4a and 4c showed antifungal activity, with compound 4a being the most active one. Compound 4a demonstrated to be fungicidal rather than fungistatic and selective activity against Cryptococcus neoformans and dermatophytes. MIC100, MIC80, and MIC50 of 4a were determ...
Source: Archiv der Pharmazie - November 19, 2009 Category: Drugs & Pharmacology Authors: Braulio Insuasty, Alexander Gutiérrez, Jairo Quiroga, Rodrigo Abonia, Manuel Nogueras, Justo Cobo, Laura Svetaz, Marcela Raimondi, Susana Zacchino Source Type: journals

2-Aryl-3-(1H-Azol-1-yl)-1H-Indole Derivatives: A New Class of Antimycobacterial Compounds - Conventional Heating in Comparison with MW-Assisted SynthesisEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
2-Aryl-3-(1H-imidazol-1-yl and 1H-1,2,4-triazol-1-yl)-1H-indole derivatives were synthesized and tested for their in-vitro antifungal and antimycobacterial activities. These indole derivatives were devoid of antifungal activity against the tested strains of Candida spp. Yet, they exhibited an interesting antitubercular activity against Mycobacterium tuberculosis reference strain H37Rv. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - November 17, 2009 Category: Drugs & Pharmacology Authors: Daniele Zampieri, Maria Grazia Mamolo, Erik Laurini, Giuditta Scialino, Elena Banfi, Luciano Vio Source Type: journals

Synthesis and Biological Evaluation of Novel 5,8-Disubstituted-2-methyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b] indoles as 5-HT6 and H1 Receptors AntagonistsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Synthesis, biological evaluation, and structure-activity relationships (SAR) for a series of novel [gamma]-carboline analogues of Dimebon are described. Among the studied compounds, tetrahydro-[gamma]-carboline 5b (2,8-dimethyl-5-[cis-2-pyridin-3-ylvinyl]-2,3,4,5-tetrahydro-carboline) has been identified as the most potent small molecule antagonist, in particular against histamine H1 and serotonin 5-HT6 receptors (IC50 < 0.45 [mu]M and IC50 = 0.73 [mu]M, respectively). A thorough comparative SAR study performed for the tested compounds has revealed significant correlations between the nature of side substituents and the re...
Source: Archiv der Pharmazie - November 17, 2009 Category: Drugs & Pharmacology Authors: Alexandre V. Ivachtchenko, Eugene B. Frolov, Oleg D. Mitkin, Volodymyr M. Kysil, Alexander V. Khvat, Sergey E. Tkachenko Source Type: journals

Arylazoamidoximes and Related Compounds as NO-modulatorsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Three amidinoarylhydrazines 1, three arylazoamidines 2, and nine arylazoamidoximes 3 have been synthesized and investigated for their potential to function as nitric oxide (NO) modulators. In-vitro studies demonstrated that 2 and 3 inhibited platelet aggregation (2c, IC50 = 3 [mu]M) which could also be shown in vivo by inhibition of thrombus formation in arterioles (3a, 22%). Moreover, for all compounds antihypertensive effects were examined in vivo with SHR rats, with 2a being the most potent candidate by lowering blood pressure by 19%. However, no common underlying mechanism of action could be shown. Some of these compou...
Source: Archiv der Pharmazie - November 17, 2009 Category: Drugs & Pharmacology Authors: Alexander Schröder, Jürke Kotthaus, Dennis Schade, Bernd Clement, Klaus Rehse Source Type: journals

Facile Synthesis and In-Vitro Antitumor Activity of Some Pyrazolo[3,4-b]pyridines and Pyrazolo[1,5-a]pyrimidines Linked to a Thiazolo[3,2-a]benzimidazole MoietyEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The key precursor E-3-(N,N-dimethylamino)-1-(3-methylthiazolo[3,2-a]benzimidazol-2-yl)prop-2-en-1-one 4 was synthesized in good yield using Gold's reagent. The reaction of enaminone 4 with 5-amino-3-aryl-1-phenylpyrazoles 5a, b in refluxing acetic acid in the presence of sulphuric acid, yielded pyrazolo[3,4-b]pyridines 7a, b. Similarly, pyrazolo[1,5-a]pyrimidines 10a, b and 14a-f were prepared by reaction of enaminone 4 with 5-amino-1H-pyrazoles 8a, b and 12a-f, respectively. The structure of pyrazolo[1,5-a]pyrimidine 10b was determined by X-ray diffraction. The synthesized compounds were tested for their in-vitro antitumo...
Source: Archiv der Pharmazie - November 17, 2009 Category: Drugs & Pharmacology Authors: Hatem A. Abdel-Aziz, Tamer S. Saleh, Heba S. A. El-Zahabi Source Type: journals

N-Malonyl-1,2-dihydroisoquinoline as a Novel Carrier for Specific Delivery of Drugs to the BrainEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
N-Malonyl-1,2-dihydroisoquinoline derivatives were synthesized and investigated as a novel carrier system for site-specific and sustained delivery of drugs to the brain. Such carriers are expected to be stable against air oxidation due to the presence of the carbonyl group close to nitrogen of the dihydroisoquinoline. Reduction of the prepared isoquinolinium quaternary derivatives with sodium dithionite afforded a novel group of N-malonyl-1,2-dihydroisoquinoline chemical delivery systems (CDS). The synthesized N-malonyl-1,2-dihydroisoquinoline chemical delivery systems were subjected to various chemical and biological inve...
Source: Archiv der Pharmazie - November 7, 2009 Category: Drugs & Pharmacology Authors: Mohamed Abdel-Aziz, Gamal El-Din A. A. Abuo-Rahma, Heba A. Hassan, Hassan H. Farag Source Type: journals

Synthesis and Antimycobacterial Activity of a Novel Series of Isonicotinylhydrazide DerivativesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
A novel series of 14 new isonicotinyl hydrazide derivatives 2a-g, 3a-g containing a 4-thiazolidinone / 2-azetidinone nucleus were synthesized by reacting N[prime]-substituted arylidene / heteroarylidene isonicotinyl hydrazide 1a-g with thioglycollic acid in the presence of dry benzene and with chloroacetyl chloride in the presence of triethylamine, respectively. Structures of all newly synthesized compounds were characterized on the basis of elemental analyses and spectral data (IR and 1H-NMR). All the title compounds were tested for their in-vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv using A...
Source: Archiv der Pharmazie - November 6, 2009 Category: Drugs & Pharmacology Authors: Sandip Jaju, Mahesh Palkar, Veeresh Maddi, Pradeepkumar Ronad, Shivalingarao Mamledesai, Darbhamulla Satyanarayana, Mangala Ghatole Source Type: journals

Protein Kinase C Activators as Synaptogenic and Memory TherapeuticsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The last decade has witnessed a rapid progress in understanding of the molecular cascades that may underlie memory and memory disorders. Among the critical players, activity of protein kinase C (PKC) isoforms is essential for many types of learning and memory and their dysfunction, and is critical in memory disorders. PKC inhibition and functional deficits lead to an impairment of various types of learning and memory, consistent with the observations that neurotoxic amyloid inhibits PKC activity and that transgenic animal models with PKC[beta] deficit exhibit impaired capacity in cognition. In addition, PKC isozymes play a...
Source: Archiv der Pharmazie - November 6, 2009 Category: Drugs & Pharmacology Authors: Miao-Kun Sun, Daniel L. Alkon Source Type: journals

Synthesis of Monomeric and Dimeric Acridine Compounds as Potential Therapeutics in Alzheimer and Prion DiseasesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Starting from substituted 9-chloroacridines, a series of quinacrine and spacered dimeric acridine compounds was prepared. Their ability to interrupt the protein association of prion- and Alzheimer-specific proteins and Ab peptides was explored using a fast screening system based on FACS analysis. The bis-acridines displayed a higher activity than the corresponding monomers. Among these derivatives, best results were obtained with the 2,4-dimethoxy-6-nitro compound 7h for A[beta]-peptides and the 2-methoxy-6-nitro compound 7f for PrP. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - November 6, 2009 Category: Drugs & Pharmacology Authors: René Csuk, Alexander Barthel, Christian Raschke, Ralph Kluge, Dieter Ströhl, Lothar Trieschmann, Gerald Böhm Source Type: journals

Synthesis and Anti-HIV-1 Integrase Activitiy of Cyano PyrimidinonesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
A series of 2-phenethyl/benzylthio-6-oxo-4-phenyl-1,6-dihydropyrimidine-5-carbonitrile were synthesized and tested against recombinant HIV-1 integrase in an enzyme assay. 2-(Phenethylthio)-4-(4-chlorophenyl)-6-oxo-1,6-dihydropyrimidine-5-carbonitrile 4m and 2-(phenethylthio)-4-(3-chlorophenyl)-6-oxo-1,6-dihydropyrimidine-5-carbonitrile 4o showed significant inhibition against integrase in the assay (strand transfer: IC50 values of 16 and 17 [mu]M, respectively). (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - November 6, 2009 Category: Drugs & Pharmacology Authors: R. Ramajayam, Nilesh B. Mahera, Nouri Neamati, Mange Ram Yadav, Rajani Giridhar Source Type: journals

Design, Synthesis, and Antifungal Activity of Novel Conformationally Restricted Triazole DerivativesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
A series of new triazole derivatives were designed and synthesized on the basis of the active site of lanosterol 14[alpha]-demethylase from Candida albicans (CACYP51). 2-(2,4-Difluorophenyl)-3-(methyl-(3-phenoxyalkyl)amino)-1-(1H-1,2,4-triazol-1-yl)propan-2-ols show excellent in-vitro activity against most of the tested pathogenic fungi. The MIC80 value of compound 8a against Candida albicans is 0.01 [mu]M, which provides a good starting template for further structural optimization. The binding modes of the designed compounds were investigated by flexible molecular docking. The compounds interacted with CACYP51 through hyd...
Source: Archiv der Pharmazie - November 6, 2009 Category: Drugs & Pharmacology Authors: Wenya Wang, Chunquan Sheng, Xiaoying Che, Haitao Ji, Zhenyuan Miao, Jianzhong Yao, Wannian Zhang Source Type: journals

Contents: Archiv der Pharmazie 11/2009Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
No Abstract. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - October 31, 2009 Category: Drugs & Pharmacology Tags: Contents Source Type: journals

Synthesis, Cytotoxicity by Bioluminescence Inhibition, Antibacterial and Antifungal Activity of ([1,2,4]Triazolo[1,5-c]quinazolin-2-ylthio)carboxylic Acid AmidesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
We report in this work the synthesis, cytotoxicity, and antimicrobial activity of ([1,2,4]triazolo[1,5-c]quinazolin-2-ylthio)carboxylic acid amides 4-7 in connection with our previous research in the preparation of triazoloquinazoline derivatives. Due to simplicity, general availability of starting materials, and high yields, the most reliable method of synthesis appeared to be the one with N,N-carbonyldiimidazole activation stage. The chemical structures of all obtained substances were deduced from FT-IR, 1H-NMR, EI-MS, and LC-MS spectral data. The results of cytotoxicity evaluated by bioluminescence inhibition of bacteri...
Source: Archiv der Pharmazie - October 30, 2009 Category: Drugs & Pharmacology Authors: Lyudmila N. Antipenko, Alexander V. Karpenko, Sergey I. Kovalenko, Andrew M. Katsev, Elena Z. Komarovska-Porokhnyavets, Vladimir P. Novikov Tags: Full Papers Source Type: journals

Relationship Between Anticancer Activity and Stereochemistry of Saldach Ligands and their Iron(III) ComplexesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
(R,R)-, (S,S)- and (R,S)-N,N[prime]-bis(salicylidene)-1,2-diaminocyclohexane (saldach) and their iron(III) complexes were screened for anticancer activity against MCF-7 and MDA-MB 231 breast cancer as well as HT-29 colon carcinoma cells. Antiproliferative effects depended on the presence of the central atom iron but were independent on the configuration at the saldach ligand. While the free ligands were inactive, the iron(III) derivatives displayed anticancer activity within a concentration range of 1 to 5 [mu]M irrespective of the used cell line. At 5 [mu]M they were even more active than cis-platin. A mode of action comp...
Source: Archiv der Pharmazie - October 30, 2009 Category: Drugs & Pharmacology Authors: Annegret Hille, Ronald Gust Tags: Full Papers Source Type: journals

Synthesis of Novel Uracil Non-Nucleoside Derivatives as Potential Reverse Transcriptase Inhibitors of HIV-1Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Novel emivirine and TNK-651 analogues 5a-d were synthesized by reaction of chloromethyl ethyl ether and / or benzyl chloromethyl ether, respectively, with uracils having 5-ethyl and 6-(4-methylbenzyl) or 6-(3,4-dimethoxybenzyl) substituents. A series of new uracil non-nucleosides substituted at N-1 with cyclopropylmethyloxymethyl 9a-d, 2-phenylethyloxymethyl 9e-h, and 3-phenylprop-1-yloxymethyl 9i-l were prepared on treatment of the corresponding uracils with the appropriate acetals 8a-c. Some of the tested compounds showed good activity against HIV-1 wild type. Among them, 1-cyclopropylmethyloxymethyl-5-ethyl-6-(3,5-dimet...
Source: Archiv der Pharmazie - October 23, 2009 Category: Drugs & Pharmacology Authors: Nasser R. El-Brollosy, Omar. A. Al-Deeb, Ali A. El-Emam, Erik B. Pedersen, Paolo La Colla, Gabriella Collu, Giuseppina Sanna, Roberta Loddo Source Type: journals

Synthesis of 2-Fluoro N10-Substituted Acridones and Their Cytotoxicity Studies in Sensitive and Resistant Cancer Cell Lines and Their DNA Intercalation StudiesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
A series of 2-fluoro N10-substituted acridone derivatives with varying alkyl side chain length with propyl, butyl substitution, and a tertiary amine group at the terminal end of the alkyl side chain were synthesized and screened against cancer cell lines SW 1573, SW 1573 2R 160 (P-gp substrate) which are non-small lung cancer cell lines, MCF-7, MCF-7/MR (BCRP substrate) are breast cancer cell lines, 2008 WT, 2008MRP1, 2008MRP2, 2008MRP3 are ovarian cancer cell lines, and human embryo kidney cell lines like HEK293, HEK293 MRP4, and HEK293 MRP5i. The propyl-series compounds showed lipophilicity in the range of 1.93 to 4.40 a...
Source: Archiv der Pharmazie - October 22, 2009 Category: Drugs & Pharmacology Authors: Yergeri C. Mayur, Zaheeruddin, Godefridus J. Peters, Clara Lemos, Ietje Kathmann, Velivela V. S. Rajendra Prasad Source Type: journals

Synthesis and Evaluation on Anticonvulsant and Antidepressant Activities of 5-Alkoxy-tetrazolo[1,5-a]quinazolinesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Several 5-alkoxy-tetrazolo[1,5-a]quinazoline derivatives have been synthesized by reacting 2,4-dichloroquinazoline with various phenols or aliphatic alcohol and then with sodium azide. The structures of these compounds have been confirmed by IR, MS, 1H-NMR, and elementary analysis. Anticonvulsant activities were evaluated using the maximal electroshock (MES) test. Most of the synthesized compounds displayed weak anticonvulsant activity at a dose of 300 mg/kg. Antidepressant activities were investigated by forced swimming test. Two compounds, namely 5-(hexyloxy)tetrazolo[1,5-a]quinazoline and 5-(4-methoxyphenoxy)tetrazolo[1...
Source: Archiv der Pharmazie - October 22, 2009 Category: Drugs & Pharmacology Authors: Huo-Jian Wang, Cheng-Xi Wei, Xian-Qing Deng, Fu-Lan Li, Zhe-Shan Quan Source Type: journals

Proline Analogue of Nitrosourea as a New Cytotoxic ProdrugEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In conclusion, carmustine and AC cause changes in the antioxidative system of normal and MOLT4 cells and are a reason of oxidative stress formation. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - October 22, 2009 Category: Drugs & Pharmacology Authors: Anna Stankiewicz-Kranc, Anna Bielawska, Krzysztof Bielawski, Elzbieta Skrzydlewska Source Type: journals

Contents: Archiv der Pharmazie 10/2009Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
No Abstract. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - September 26, 2009 Category: Drugs & Pharmacology Tags: Contents Source Type: journals

Synthesis and Biological Evaluation of 2-Mercapto-1,3-benzothiazole Derivatives with Potential Antimicrobial ActivityEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The enhancement of bacterial resistance of pathogens to currently available antibiotics constitutes a serious public health threat. So, intensive efforts are underway worldwide to develop new antimicrobial agents. To identify compounds with a potent antimicrobial profile, we designed and synthesized low molecular weight 2-mercaptobenzothiazole derivatives 2a-2l and 3a-3l. Both series were screened for in-vitro antibacterial activity against the representative panel of Gram-positive and Gram-negative bacteria strains. The biological screening identified compounds 2e and 2l as the most active ones showing an interesting anti...
Source: Archiv der Pharmazie - September 14, 2009 Category: Drugs & Pharmacology Authors: Carlo Franchini, Marilena Muraglia, Filomena Corbo, Marco Antonio Florio, Antonia Di Mola, Antonio Rosato, Rosanna Matucci, Marta Nesi, Francoise van Bambeke, Cesare Vitali Source Type: journals

Synthesis and Cytotoxic Evaluation of 6-(3-Pyrazolylpropyl) Derivatives of 1,4-Naphthohydroquinone-1,4-diacetateEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Several new 6-(3-pyrazolylpropyl) derivatives of 1,4-naphthohydroquinone-1,4-diacetate (NHQ-DA) have been prepared by chemical modifications of the Diels-Alder adduct of [alpha]-myrcene and 1,4-benzoquinone. All these new compounds and precursors have been evaluated in vitro for their cytotoxicity against cultured human cancer cells of MB-231 breast-adeno carcinoma, A-549 lung carcinoma, and HT-29 colon carcinoma. GI50 values ranged in and below the micromolar concentration level. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - September 13, 2009 Category: Drugs & Pharmacology Authors: Aurora Molinari, Alfonso Oliva, Claudia Ojeda, José M. Miguel del Corral, M. Angeles Castro, Carmen Cuevas, Arturo San Feliciano Source Type: journals

Synthesis and In-vitro Activity of 4[prime]-Modified Analogues of ddA as Potent Anti-HIV AgentsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This paper reports the synthesis of novel 4[prime]-hydrophobic pocket deoxythreosyl C-nucleosides. The key threose-like intermediates 9 and 14 were constructed from acyclic ketone derivatives, respectively. The antiviral activities of the synthesized compounds against the HIV-1, HSV-1, HSV-2, and HCMV viruses were evaluated. The 9-deaza-adenine derivatives 10 and 20 showed good anti-HIV activity without exhibiting significant cytotoxicity. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - September 13, 2009 Category: Drugs & Pharmacology Authors: Joon Hee Hong, Chang Hyun Oh Source Type: journals

Contents: Archiv der Pharmazie 9/2009Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
No Abstract. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - August 31, 2009 Category: Drugs & Pharmacology Tags: Contents Source Type: journals

Synthesis and Pharmacological Evaluation of Thiazole and Isothiazole Derived ApomorphinesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
We have presented the synthesis of novel thiazolo- and isothiazolo-apomorphines 12-17 resulting-in part-from an unexpected isomerization step occurred during the acid-catalyzed rearrangement of precursor thiazolo-morphinandienes 3-5. These 2,3-disubstituted apomorphines represent a new group of A-ring substituted aporphines. The receptor binding studies revealed that with the exception of two derivatives all the tested compounds have limited affinity for dopamine-receptor subtypes. Functional calcium assay for the most active isothiazolo-apomorphine showed higher affinities for D1 and D2L subtypes. The docking of these lig...
Source: Archiv der Pharmazie - August 27, 2009 Category: Drugs & Pharmacology Authors: Attila Sipos, Franziska K. U. Mueller, Jochen Lehmann, Sándor Berényi, Sándor Antus Source Type: journals

Synthesis and Cytotoxicity Studies of New Cryptophycin AnaloguesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Two analogues of cryptophycin were synthesized and biologically evaluated for their in-vitro cytotoxicities against several solid tumors and leukemia cell lines. The results revealed that both analogues exhibited a broad range of cytotoxic activity with observed IC50 values in the [mu]M-range, and compound 4 was more effective than compound 3 in most assays studied. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - August 26, 2009 Category: Drugs & Pharmacology Authors: Wen Lu Liu, Jian Cun Zhang, Fa Qin Jiang, Lei Fu Source Type: journals

Synthesis and Biological Evaluation of Some Polymethoxylated Fused Pyridine Ring Systems as Antitumor AgentsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
A series of 3,5-bis(arylidene)-4-piperidones like chalcone analogues carrying variety of methoxylated aryl groups, pyrazolo[4,3-c]pyridines, pyrido[4,3-d]pyrimidines, and pyrido[3,2-c]pyridines, carrying an arylidene moiety, and some pyrano[3,2-c]pyridines, like flavone and coumarin isosteres, were synthesized and screened for their in-vitro antitumor activity at the National Cancer Institute (NCI, USA). The tested compounds 7, 9, 10, 12, 13, 15, 17, and 19 exhibited a broad spectrum of antitumor activity. Compounds belonging to the pyrazolo[4,3-c]pyridine series proved to be more active than those of the pyrido[3,2-c]pyri...
Source: Archiv der Pharmazie - August 26, 2009 Category: Drugs & Pharmacology Authors: Sherif A. F. Rostom, Ghada S. Hassan, Hussein I. El-Subbagh Source Type: journals

Antitumoractive Endoperoxides from TriterpenesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
A series of triterpene endoperoxides was synthesized and screened for antitumor activity in a panel of 15 human cancer cell lines by a sulforhodamine-B (SRB) assay. The compounds induce apoptosis and show excellent antitumor activity. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - August 24, 2009 Category: Drugs & Pharmacology Authors: Anja Niesen, Alexander Barthel, Ralph Kluge, Alexander Köwitzsch, Dieter Ströhl, Stefan Schwarz, René Csuk Source Type: journals

Synthesis and Anti-HIV-1 Activity of 1-Substiuted 6-(3-Cyanobenzoyl) and [(3-Cyanophenyl)fluoromethyl]-5-ethyl-uracilsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
1-Substiuted 6-(3-cyanobenzoyl) and [(3-cyanophenyl)fluoromethyl]-5-ethyl-uracils were synthesized and evaluated in cell-based assays against HIV-1 wild-type and its clinically relevant non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant mutants. Some of the synthesized compounds showed activity against HIV-1 wild-type in the same range as Emivirine (MKC-442). 3-{[3-(Allyloxymethyl)-5-ethyl-2,6-dioxo-1,2,3,6-tetrahydropyrimidin-4-yl]fluoromethyl}-benzonitrile 11b showed moderate activity against the Y181C HIV-1 mutant strain. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - July 26, 2009 Category: Drugs & Pharmacology Authors: Yasser M. Loksha, Erik B. Pedersen, Roberta Loddo, Paolo La Colla Source Type: journals

Synthesis and In-Vitro Anti-Hepatitis-B Virus Activity of 6H-[1]Benzothiopyrano[4,3-b] quinolin-10-olsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
A series of 9-methoxy-6H-[1]benzothiopyrano[4,3-b]quinolin-10-ols with a Mannich side chain were synthesized and evaluated for their anti-Hepatitis B virus (HBV) activity in HepG2.2.15 cells. Some compounds showed significant anti-HBV activity with IC50 values less than 41 [mu]M. Among them, compound 9b was the most effective anti-HBV agent (IC50 = 1.7 [mu]M, SI = 60.3). (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - July 26, 2009 Category: Drugs & Pharmacology Authors: Wei Jia, Yanfang Zhao, Rongdong Li, Yanjiao Wu, Zebiao Li, Ping Gong Source Type: journals

Novel l[beta]-Methylcarbapenems Having Cyclic Sulfonamide Moieties: Synthesis and Evaluation of in-vitro Biological Activity - Part IIEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The synthesis of a new series of 1[beta]-methylcarbapenems having cyclic sulfonamide moieties is described. Their in-vitro antibacterial activities against both Gram-positive and Gram-negative bacteria were tested and the effect of a substituent on the pyrrolidine ring was investigated. One particular compound IIIe having a [1,2,5]thiadiazolidin 1,1-dioxide moiety showed the most potent antibacterial activity. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - July 13, 2009 Category: Drugs & Pharmacology Authors: Seong Jong Kim, Jung-Hyuck Cho, Chang-Hyun Oh Source Type: journals

3-Imidazolyl-Substituted Flavans as Potential Antifungal Agents: Synthesis, Stereochemical Properties, and Antifungal ActivityEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
A new series of 3-imidazolyl-substituted flavan derivatives being equipped with a N-(phenethyl)-azole scaffold as the common pharmacophore of azole antifungals, were synthesized. The stereochemical and conformational properties of compounds were also characterized by 1H-NMR data. The results of the antifungal evaluation of trans-3-imidazolyl-substituted flavan-4-ones and (Z)-trans-3-imidazolyl-substituted flavan-4-one oximes in comparison with the reference drug fluconazole indicated that most target compounds possessed significant in-vitro antifungal activities against the tested fungi, comparable or superior to fluconazo...
Source: Archiv der Pharmazie - July 13, 2009 Category: Drugs & Pharmacology Authors: Saeed Emami, Alireza Foroumadi Source Type: journals

Synthesis of (1R,2R)- and (1S,2R)-1,2-Epoxy-3-hydroxypropylphosphonates as Analogues of FosfomycinEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Cyclohexylammonium (1R,2R)-1,2-epoxy-3-hydroxypropylphosphonate was conveniently synthesized from dibenzyl (1S,2R)-2,3-O-cyclohexylidene-1,2,3-trihydroxypropylphosphonate by a reaction sequence including mesylation, hydrolysis of acetal, intramolecular Williamson reaction, and hydrogenation in the presence of cyclohexylamine. For dibenzyl (1S,2R)-2,3-O-cyclohexylidene-1,2,3-trihydroxypropylphosphonates the same approach was not successful, since prior the epoxide-ring closure tritylation of HO-C3 in dibenzyl (1R,2R)-2,3-dihydroxy-1-mesyloxypropylphosphonate was necessary and the hydrogenolysis of dibenzyl (1S,2R)-1,2-epoxy...
Source: Archiv der Pharmazie - July 13, 2009 Category: Drugs & Pharmacology Authors: Andrzej E. Wróblewski, Eligia M. Szewczyk, Irena I. Baôk-Sypie[nacute] Source Type: journals

6-Substituted Indolo[1,2-c]quinazolines as New Antimicrobial AgentsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
A series of 2-o-arylidineaminophenylindoles and their cyclic derivatives (indolo[1,2-c]quinazolines) were synthesized. The reactions occurred under relatively mild conditions and afforded the desired product in good yields. Molecular structures of the synthesized compounds were confirmed by IR, 1H-NMR, 13C-NMR, MS spectra, and elemental analyses. Furthermore, all the final products were screened for in-vitro antibacterial activity against three Gram-positive and three Gram-negative bacteria and also tested for their inhibitory action against three strains of fungi. Compound IIc showed potent activity against all the bacter...
Source: Archiv der Pharmazie - July 13, 2009 Category: Drugs & Pharmacology Authors: Rondla Rohini, Kanne Shanker, P. Muralidhar Reddy, Vasam Chandra Sekhar, Vadde Ravinder Source Type: journals

Synthesis and Characterization of New Liver Targeting 5-Fluorouracil-Cholic Acid ConjugatesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The objective of this work was to develop a liver-specific antihepato carcinoma agent. A series of 5-fluorouracil / cholic acid conjugates (5-FU-cholic acid conjugates) were prepared and tested for their chemical characteristics and bio-distribution properties. The in-vitro stability trial showed 5-FU-cholic acid conjugates could be completely hydrolyzed by heating at 70°C in an acidic solution, pH = 1, for 5 min. The fast and complete hydrolysis of these compounds could be compatible with a fast separation and analysis method to shorten the analysis time. The decomposition speeds of the 5-FU-cholic acid conjugates in dif...
Source: Archiv der Pharmazie - July 13, 2009 Category: Drugs & Pharmacology Authors: Shan Qian, Jian-Bo Wu, Xiao-Chun Wu, Jie Li, Yong Wu Source Type: journals

Benzothiazole Incorporated Barbituric Acid Derivatives: Synthesis and Anticonvulsant ScreeningEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
A series of 1-(6-substituted-1,3-benzothiazol-2-yl)-3-(substituted phenyl)hexahydro-2,4,6-pyrimidinetriones 4a-t were synthesized starting from substituted anilines. These compounds contained two active anticonvulsant pharmacophores, benzothiazole and barbituric acid. Structures of the compounds were confirmed on the basis of different spectroscopic techniques. All the compounds were evaluated for their anticonvulsant activity. Three compounds 4c, 4d, and 4s showed promising anticonvulsant activities in Maximal Electroshock Seizure test (MES) and subcutaneous pentylenetetrazole test (scPTZ). They also displayed a wide safe...
Source: Archiv der Pharmazie - June 29, 2009 Category: Drugs & Pharmacology Authors: Nadeem Siddiqui, Waquar Ahsan Source Type: journals

Synthesis of Dimeric Quinazolin-2-one, 1,4-Benzodiazepin-2-one, and Isoalloxazine Compounds as Inhibitors of Amyloid Peptides AssociationEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The synthesis of dimeric compounds derived from quinazolin-2-one and 1,4-benzodiazepin-2-one possessing a piperazine or homopiperazine spacer was investigated. In addition, a piperazine spacered bis-isoalloxazine and a bis-riboflavin compound were prepared and their ability to interrupt the association of prion proteins and Alzheimer-specific A[beta] peptides was investigated using a fast screening system based on flow cytometry. The bis-isoalloxazine 14 was identified as a new lead structure. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - June 28, 2009 Category: Drugs & Pharmacology Authors: Alexander Barthel, Lothar Trieschmann, Dieter Ströhl, Ralph Kluge, Gerald Böhm, René Csuk Source Type: journals

Synthesis of Novel 2,5-Disubstituted 1,3,4-Thiadiazoles for Their Potential Anticonvulsant Activity: Pharmacophoric Model StudiesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
A series of novel N1-[5-(4-substituted phenyl)-1,3,4-thiadiazol-2-yl]-N4-(4-substituted benzaldehyde)-semicarbazone 1-12, N1-[5-(4-substituted phenyl)-1,3,4-thiadiazol-2-yl]-N4-[1-(4-substituted phenyl)ethanone]-semicarbazone 13-16, and N1-[5-(4-substituted phenyl)-1,3,4-thiadiazol-2-yl]-N4-[1-(4-substituted phenyl) (phenyl) methanone]-semicarbazone 17-20 were synthesized for their anticonvulsant activity. The chemical structures of the compounds were proved by elemental and spectral (IR, 1H-NMR, 13C-NMR, and MS) analysis. The anticonvulsant potential of the compounds was investigated using maximal electroshock seizure (ME...
Source: Archiv der Pharmazie - June 28, 2009 Category: Drugs & Pharmacology Authors: Harish Rajak, Ravitas Deshmukh, Navneet Aggarwal, Sushil Kashaw, Murli Dhar Kharya, Pradeep Mishra Source Type: journals

Multi-Component Synthesis of Dihydropyrimidines by Iodine Catalyst at Ambient Temperature and in-vitro Antimycobacterial ActivityEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
An efficient and simple three-component domino synthesis of some new dihydropyrimidines (DHPMs) from aromatic aldehydes, 1,3-dicarbonyl compounds and N-(3-chloro-4-fluorophenyl)urea using molecular iodine as catalyst is described. The 1-substituted dihydropyrimidines were isolated in good to excellent yields (78-90%) within a short reaction time (4-6 h) at ambient temperature. The biological evaluation revealed that the newly synthesized compounds (4a-i and 5a-i) exhibited moderate antimycobacterial activity against Mycobacterium tuberculosis H37 RV. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - June 28, 2009 Category: Drugs & Pharmacology Authors: Paresh Zalavadiya, Satish Tala, Jignesh Akbari, Hitendra Joshi Source Type: journals

Synthesis and Cytotoxic Activity of Novel Amidine Analogues of Bis(2-chloroethyl)amineEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Novel nitrogen mustard agents 7-12 involving 4-(N,N-bis(2-chloroethyl)aminophenyl)propylamine linked to a 5-(4-N-alkylamidinophenyl)-2-furancarboxylic acid moiety by the formation of an amide bond have been synthesized, characterized, and evaluated for their in-vitro cytotoxic activity against MDA-MB-231 and MCF-7 human breast cancer cells. Evaluation of the cytotoxicity of 7-12 employing a MTT assay and inhibition of [3H]thymidine incorporation into DNA demonstrated that these compounds exhibit remarkable cytotoxic effects in comparison with 4-[bis(2-chloroethyl)amino]benzenebutanoic acid. Compounds 7 and 9, which possess...
Source: Archiv der Pharmazie - June 28, 2009 Category: Drugs & Pharmacology Authors: Krzysztof Bielawski, Anna Bielawska, Bozena Poplawska Source Type: journals

Synthesis and Anti-Inflammatory Activity of Novel (4-Hydroxyphenyl)(2,4-dimethoxyphenyl) Methanone DerivativesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
In the scope of the research program aiming to perform the synthesis and pharmacological evaluation of novel possible anti-inflammatory compounds, in this manuscript, we report the synthesis of novel carboxamide 9a-d and thioamide 10a-d derivatives from the benzophenone and piperidine nucleus. Variation in the functional group at the N-terminal of piperidine led to two sets of compounds, bearing the carboxamide and thioamide, respectively. The characterization of this new class of compounds was performed with 1H-NMR, LC-MS, IR, and elemental analysis. The newly synthesized compounds were screened for their anti-inflammator...
Source: Archiv der Pharmazie - June 12, 2009 Category: Drugs & Pharmacology Authors: Kambappa Vinaya, Raja Naika, Channappillekoppal S. Ananda Kumar, Somasagara R. Ranganath, Salekoppal B. Benaka Prasad, Venkatarangaiah Krishna, Kanchugarakoppal S. Rangappa Source Type: journals

Synthesis, in-vitro Microbial and Cytotoxic Studies of New Benzimidazole DerivativesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Several new classes of benzimidazole derivatives were synthesized and evaluated for in-vitro antimicrobial and cytotoxic activities. The results showed that all synthesized compounds exhibited moderate antimicrobial activity, and compounds 2, 4, and 13 displayed cytotoxic activity (as LD50) at the concentration 1×10-3 M against Artemia salina. (Source: Archiv der Pharmazie)
Source: Archiv der Pharmazie - June 10, 2009 Category: Drugs & Pharmacology Authors: Reddy S. Harisha, Kallappa M. Hosamani, Rangappa S. Keri Source Type: journals

Synthesis, Antiviral and Cytostatic Evaluation of Unsaturated Exomethylene and Keto D-Lyxopyranonucleoside AnaloguesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This report describes the synthesis of unsaturated exomethylene lyxopyranonucleoside analogues as potential biologically active agents. Commercially available 1,2,3,4-tetra-O-acetyl-[alpha]-D-lyxopyranose 1 was condensed with silylated thymine and uracil, respectively, deacetylated and acetalated to afford 1-(2,3-O-isopropylidene-[alpha]-D-lyxopyranosyl)thymine 4a and 1-(2,3-O-isopropylidene-[alpha]-D-lyxopyranosyl)uracil 4b. The new derivatives 1-(2,3,4-trideoxy-4-methylene-[alpha]-pent-2-enopyranosyl)thymine 8a and 1-(2,3,4-trideoxy-4-methylene-[alpha]-pent-2-enopyranosyl)uracil 8b were prepared via two different key int...
Source: Archiv der Pharmazie - May 30, 2009 Category: Drugs & Pharmacology Authors: Niki Tzioumaki, Evangelia Tsoukala, Stella Manta, George Agelis, Jan Balzarini, Dimitri Komiotis Source Type: journals

Pyrazolo[3,4-d]pyrimidine Derivatives as COX-2 Selective Inhibitors: Synthesis and Molecular Modelling StudiesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
The pyrazolo[3,4-d]pyrimidine system shows a multitude of interesting pharmacological properties. Owing to the potential anti-inflammatory activity of 5-benzamido-pyrazolo[3,4-d]pyrimidin-4-one derivatives and considering the easy synthesis of this class of compounds, a set of new 5-benzamido-1H-pyrazolo[3,4-d]pyrimidin-4-ones has been prepared in 42-80% yields by reacting 5-aminopyrazole-4(N-benzoyl)carbohydrazide derivatives and the opportune triethylorthoesters. Compounds 8a, b, 10a-d, and 11a, b revealed a superior inhibitory profile against COX-2, when compared to that of reference standards NS398 and indomethacin. Mo...
Source: Archiv der Pharmazie - May 28, 2009 Category: Drugs & Pharmacology Authors: Demetrio Raffa, Benedetta Maggio, Fabiana Plescia, Stella Cascioferro, Maria Valeria Raimondi, Salvatore Plescia, Maria Grazia Cusimano Source Type: journals

Synthesis and Antibacterial Activity of a New Series of 3-[3-(Substituted Phenyl)-1-Isonicotinoyl-1H-Pyrazol-5-yl]-2H-Chromen-2-one DerivativesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
A novel series of 3-[3-(substituted phenyl)-1-isonicotinoyl-1H-pyrazol-5-yl]-2H-chromen-2-one derivatives 4a-k have been synthesized by the reaction of 3-[2,3-dibromo-3-(substituted phenyl) propanoyl]-2H-chromen-2-one 3a-k and isonicotinic acid hydrazide in the presence of triethylamine in absolute ethanol, characterized by spectral data and screened for their in-vitro antibacterial activity against Gram-positive and Gram-negative bacteria. Among the series, compounds 4e, 4i, and 4k displayed an encouraging antibacterial activity profile as compared to the reference drug ampicillin against tested bacterial strains. (Source...
Source: Archiv der Pharmazie - May 27, 2009 Category: Drugs & Pharmacology Authors: Prashant Aragade, Veeresh Maddi, Suresh Khode, Mahesh Palkar, Pradeepkumar Ronad, Shivalingarao Mamledesai, Darbhamulla Satyanarayana Source Type: journals

Generation and Evaluation of a Homology Model of PfGSK-3Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Plasmodial GSK-3 is a potential new target for malaria therapy. For a structure-based design project, the three-dimensional information of the designated target is needed. Unfortunately, experimental structure data for plasmodial GSK-3 is not yet available. Homology building can be used to generate such three-dimensional structure data using structure information of a homologous protein. GSK-3 possesses a very flexible ATP-binding site, a fact reflected in the variety of X-ray structures of the human GSK-3[beta] which are deposited in the protein data base and are crystallized with different ligands. We used ten different ...
Source: Archiv der Pharmazie - May 27, 2009 Category: Drugs & Pharmacology Authors: Sebastian Kruggel, Thomas Lemcke Source Type: journals

Synthesis and pp60c-Src Tyrosine Kinase Inhibitory Activities of Novel Indole-3-Imine and Amine Derivatives Substituted at N1 and C5Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
A series of novel 1,3,5-trisubstituted indole derivatives, namely, N-benzyl 5-phenyl indole-3-imine, N-benzyl-5-(p-fluorophenyl)indole-3-imine and their corresponding amine congeners, were designed and synthesized as pp60c-Src tyrosine kinase inhibitors, and their inhibitory activities toward pp60c-Src tyrosine kinase were evaluated by in-vitro kinase assay. Pre-screening at two doses of compounds against kinase target revealed that, except for the N-benzyl-5-phenyl indole imine derivatives 7a-7d, all indole derivatives show the target inhibition at varying levels. Consequently, the compounds, 8c, 8f, 8g, and 8h, were sele...
Source: Archiv der Pharmazie - May 27, 2009 Category: Drugs & Pharmacology Authors: Zuhal Kiliç, Yasemin G. Isgör, Süreyya Ölgen Source Type: journals

Synthesis and Biological Evaluation of Some Novel Polysubstituted Pyrimidine Derivatives as Potential Antimicrobial and Anticancer AgentsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Synthesis and evaluation of the antimicrobial and cytotoxic activity of two series of polysubstituted pyrimidines comprising the thioether functionality and other pharmacophores, reported to contribute to various chemotherapeutic activities are described. All newly synthesized compounds were subjected to in-vitro antibacterial and antifungal screening. Out of the compounds tested, 18 derivatives displayed an obvious inhibitory effect on the growth of the tested Gram-positive and Gram-negative bacterial strains, with special effectiveness against the Gram-positive strains. Compounds 1, 2, 6, 7, 9, 10, 11, 21, and 24 reveale...
Source: Archiv der Pharmazie - May 7, 2009 Category: Drugs & Pharmacology Authors: Sherif A. F. Rostom, Hayam M. A. Ashour, Heba A. Abd El Razik Source Type: journals

Synthesis and Studies of New 2-(Coumarin-4-yloxy)-4,6-(substituted)-s-Triazine Derivatives as Potential Anti-HIV AgentsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Novel 2-(coumarin-4-yloxy)-4,6-(substituted)-s-triazine derivatives i. e., diaryltriazine (DATA) are reported as novel non-nucleoside reverse transcriptase inhibitors (NNRTIs), were synthesized and their activities against human immunodeficiency virus HIV-1 (III-B), HIV-2 (ROD), and the double RT mutant HIV-1 (K103N and Y181C) were assessed. Modifications at positions 4 and 6 of the coumarinyl-triazine scaffold generated interesting derivatives displaying good to moderate anti-HIV activity against selected HIV strains as compared to nevirapine and efavirenz. The synthesized compounds were characterized by FTIR, 1H-NMR, and...
Source: Archiv der Pharmazie - May 4, 2009 Category: Drugs & Pharmacology Authors: Dharmesh H. Mahajan, Christophe Pannecouque, Erik De Clercq, Kishor H. Chikhalia Source Type: journals