Archiv der Pharmazie
Copyright © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
Edited By: Holger Stark
Impact Factor: 1.396
ISI Journal Citation Reports © Ranking: 2013: 42/58 (Chemistry Medicinal); 74/148 (Chemistry Multidisciplinary); 180/256 (Pharmacology & Pharmacy)
Online ISSN: 1521-4184
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Recently Published Articles
- Novel 4-Thiazolidinones as Non-Nucleoside Inhibitors of Hepatitis C Virus NS5B RNA-Dependent RNA Polymerase
Gizem Çakır, İlkay Küçükgüzel, Rupa Guhamazumder, Esra Tatar, Dinesh Manvar, Amartya Basu, Bhargav A. Patel, Javairia Zia, Tanaji T. Talele and Neerja Kaushik-Basu
Article first published online: 2 DEC 2014 | DOI: 10.1002/ardp.201400247
Novel 5-arylidene-4-thiazolidinones 29–42 together with their synthetic precursors 22–28 were tested for hepatitis C virus NS5B inhibitory activity. Compound 33, an arylidene derivative, was found to be the most active compound in this series, with an IC50 value of 25.3 µM. Molecular docking studies were performed on the thumb pocket-II of NS5B to postulate the binding mode for these compounds.
- Design, Synthesis, and Evaluation of Non-ATP-Competitive Small-Molecule Polo-Like Kinase 1 (Plk1) Inhibitors
Dong-Xing Chen, Jie Huang, Meng Liu, Yun-Gen Xu and Cheng Jiang
Article first published online: 27 NOV 2014 | DOI: 10.1002/ardp.201400294
A series of small-molecule Plk1 inhibitors were identified through rational design according to the substrate-binding pocket of Plk1. The best compound 5i showed Plk1 inhibitory activity with an IC50 value of 0.68 μM and HeLa cell growth inhibitory activity with an IC50 value of 0.51 μM. Compound 5i proved to be an ATP-independent and substrate-dependent Plk1 inhibitor.
- A New Series of Antibacterial Nitrosopyrimidines: Synthesis and Structure–Activity Relationship
Monica Olivella, Antonio Marchal, Manuel Nogueras, Manuel Melguizo, Beatriz Lima, Alejandro Tapia, Gabriela E. Feresin, Oscar Parravicini, Fernando Giannini, Sebastián A. Andujar, Justo Cobo and Ricardo D. Enriz
Article first published online: 21 NOV 2014 | DOI: 10.1002/ardp.201400271
A new series of nitrosopyrimidines possessing strong antibacterial activity were synthesized. A detailed structure–activity relationship study, supported by theoretical calculations, helped to identify the minimal structural requirements for the antibacterial action of the new nitrosopyrimidines.
- Monte Carlo Method-Based QSAR Modeling of Penicillins Binding to Human Serum Proteins
Jovana B. Veselinović, Andrey A. Toropov, Alla P. Toropova, Goran M. Nikolić and Aleksandar M. Veselinović
Article first published online: 18 NOV 2014 | DOI: 10.1002/ardp.201400259
The binding of penicillins to human serum proteins was modeled with optimal descriptors based on SMILES notation. The Monte Carlo method was used as a chemoinformatic tool to build the QSAR model, which was finally applied to demonstrate the possibility of designing new penicillin derivatives with desired binding properties.
- Design and Synthesis of Benzimidazole Analogs Endowed with Oxadiazole as Selective COX-2 Inhibitor (pages 923–935)
Ankita Rathore, Mujeeb Ur Rahman, Anees Ahamad Siddiqui, Abuzer Ali and Mohammad Shaharyar
Article first published online: 9 OCT 2014 | DOI: 10.1002/ardp.201400219
A new series of benzimidazole molecules bearing oxadiazole were synthesized from 2-(2-((pyrimidin-2-ylthio)methyl)-1H-benzo[d]-imidazol-1-yl)acetohydrazide and screened in vitro for their COX-1 and COX-2 inhibitory potencies. One of the new compounds may serve as a lead for developing new COX-2 inhibitors.