Archiv der Pharmazie

Cover image for Vol. 348 Issue 3

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. 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).

  2. 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.

  3. 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.

  4. New Benzo[d]thiazol-2-yl-aminoacetamides as Potential Anticonvulsants: Synthesis, Activity and Prediction of Molecular Properties

    Ruhi Ali and Nadeem Siddiqui

    Article first published online: 17 MAR 2015 | DOI: 10.1002/ardp.201400466

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    New N-(substituted-2-oxo-4-phenylazetidin-1-yl)-2-((6-substitutedbenzo[d]thiazol-2-yl)amino)acetamide derivatives were synthesized and screened for anticonvulsant activity (MES and scPTZ tests). Two of the compounds, 5b and 5q, with promising ED50 values of 15.4 and 18.6 mg/kg, respectively, may act as lead compounds. The pharmacokinetic profiles of all the synthesized compounds were estimated by Molinspiration software.

  5. Antimicrobial and Antiquorum-Sensing Studies. Part 3: Synthesis and Biological Evaluation of New Series of [1,3,4]Thiadiazoles and Fused [1,3,4]Thiadiazoles

    Nadia S. El-Gohary and Mona I. Shaaban

    Article first published online: 13 MAR 2015 | DOI: 10.1002/ardp.201400381

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    New series of [1,3,4]thiadiazoles and fused [1,3,4]thiadiazoles were synthesized and screened for their antibacterial activity against Staphylococcus aureus, Bacillus cereus, and Escherichia coli, as well as their antifungal activity against Candida albicans and Aspergillus flavus 3375. The compounds were also examined for their antiquorum-sensing activity against Chromobacterium violaceum ATCC 12472. Compounds 3b and 10a showed interesting activity in all assays.