Archiv der Pharmazie

Cover image for Vol. 348 Issue 4

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. Synthesis and Biological Evaluation of Some New 2,5-Substituted 1-Ethyl-1H-benzoimidazole Fluorinated Derivatives as Direct Thrombin Inhibitors

    Meilin Li and Yujie Ren

    Article first published online: 30 MAR 2015 | DOI: 10.1002/ardp.201400463

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    A new series of fluorinated derivatives were evaluated for their in vitro thrombin inhibition activities. 3-({2-[(4-Carbamimidoyl-2-fluoro-phenylamino)-methyl]-1-ethyl-1H-benzoimidazole-5-carbonyl}-pyridin-2-yl-amino)-propionic acid 14h shows the most potent antithrombin activity (IC50 = 3.39 nM). Molecular docking revealed that its inhibition mode was similar to that of dabigatran.

  2. Synthesis of Carbamide Derivatives Bearing Tetrahydroisoquinoline Moieties and Biological Evaluation as Analgesia Drugs in Mice

    Qianqian Qiu, Jingjie Wang, Xin Deng, Hai Qian, Haiyan Lin and Wenlong Huang

    Article first published online: 30 MAR 2015 | DOI: 10.1002/ardp.201400455

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    A novel carbamide derivative of tetrahydroisoquinoline I 1 had impressive TRPV1 antagonism activity (89.02%), exerting potency similarity with the positive control BCTC. Moreover, in mice, I 1 could significantly inhibit the reaction to pain and nociception in three different pain models, and trigger the analgesic activity in a dose-dependent manner.

  3. 9H-Carbazole Derivatives Containing the N-Benzyl-1,2,3-triazole Moiety as New Acetylcholinesterase Inhibitors

    Hamidreza Akrami, Bibi F. Mirjalili, Mehdi Khoobi, Alireza Moradi, Hamid Nadri, Saeed Emami, Alireza Foroumadi, Mohsen Vosooghi and Abbas Shafiee

    Article first published online: 27 MAR 2015 | DOI: 10.1002/ardp.201400365

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    A series of triazole-containing carbazoles were prepared via one-pot three-component click reaction. The in vitro anti-acetylcholinesterase assay showed that the 2-methylbenzyl derivative 6c was the most active compound (IC50 = 1.93 µM).

  4. Recent Progress on Pyrazole Scaffold-Based Antimycobacterial Agents

    Rangappa S. Keri, Karam Chand, Thippeswamy Ramakrishnappa and Bhari Mallanna Nagaraja

    Article first published online: 27 MAR 2015 | DOI: 10.1002/ardp.201400452

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    Due to resistance to conventional antibiotics there is a need for new therapeutic strategies to combat Mycobacterium tuberculosis. Published reports on the pyrazole core are collated to provide an overview so that its full therapeutic potential for the treatment of tuberculosis (TB) becomes clear. Possible structure–activity relationships of pyrazole analogs are discussed for designing better anti-TB agents.

  5. N-(2-(Piperazin-1-yl)phenyl)arylamide Derivatives as β-Secretase (BACE1) Inhibitors: Simple Synthesis by Ugi Four-Component Reaction and Biological Evaluation

    Najmeh Edraki, Omidreza Firuzi, Yousef Fatahi, Mohammad Mahdavi, Mehdi Asadi, Saeed Emami, Kouros Divsalar, Ramin Miri, Aida Iraji, Mehdi Khoshneviszadeh, Loghman Firoozpour, Abbas Shafiee and Alireza Foroumadi

    Article first published online: 19 MAR 2015 | DOI: 10.1002/ardp.201400322

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    A novel series of N-(2-(piperazin-1-yl)phenyl)aryl carboxamide derivatives were simply synthesized by Ugi-multicomponent reaction as β-secretase (BACE1) inhibitors. Compound 14 (R1 = indol-3-yl, R2 = 2-thienyl) showed superior BACE1 inhibition at 10 and 40 µM.