Archiv der Pharmazie

Cover image for Vol. 347 Issue 12

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

  1. Design, Synthesis, and Biological Evaluation of Novel 2H-Pyran-2-one Derivatives as Potential HIV-1 Reverse Transcriptase Inhibitors

    Andrea Defant, Ines Mancini, Rossella Tomazzolli and Jan Balzarini

    Article first published online: 19 DEC 2014 | DOI: 10.1002/ardp.201400235

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    Twenty-one potential non-nucleoside reverse transcriptase inhibitors with 2H-pyran-2-one hybrid structures based on the natural product (+)-calanolide A and the synthetic molecule α-APA, known as potent and selective inhibitors of HIV replication, were synthesized by a convergent strategy and tested against HIV-infected CEM cell cultures. Only one molecule displayed a modest activity whereas some others showed not easily predictable cytotoxic effects.

  2. 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

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    Novel 5-arylidene-4-thiazolidinones 2942 together with their synthetic precursors 2228 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.

  3. 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

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    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.

  4. 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

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    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.

  5. 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

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    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.