Archiv der Pharmazie

Cover image for Vol. 348 Issue 8

Edited By: Holger Stark

Impact Factor: 1.531

ISI Journal Citation Reports © Ranking: 2014: 41/59 (Chemistry Medicinal); 75/157 (Chemistry Multidisciplinary); 179/254 (Pharmacology & Pharmacy)

Online ISSN: 1521-4184

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Recently Published Articles

  1. Synthesis and Screening of Human Monoamine Oxidase-A Inhibitor Effect of New 2-Pyrazoline and Hydrazone Derivatives

    Begüm Evranos-Aksöz, İpek Baysal, Samiye Yabanoğlu-Çiftçi, Teodora Djikic, Kemal Yelekçi, Gülberk Uçar and Rahmiye Ertan

    Article first published online: 21 AUG 2015 | DOI: 10.1002/ardp.201500212

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    New 2-pyrazoline and hydrazone derivatives were synthesized as potential human monoamine oxidase (hMAO) inhibitors. Most of the compounds were found to be competitive, reversible, and selective inhibitors of hMAO-A/B. 6i, 6d, and 6a exhibited the highest inhibitory activity toward hMAO-A, and 3-(3,5-dichloro-2-hydroxyphenyl)-5-m-tolyl-4,5-dihydropyrazole-1-yl)(furane-2-yl)methanone (5c) showed higher selectivity than moclobemide, a known potent MAO-A inhibitor.

  2. Synthesis of Tolmetin Hydrazide–Hydrazones and Discovery of a Potent Apoptosis Inducer in Colon Cancer Cells

    Ş. Güniz Küçükgüzel, Derya Koç, Pelin Çıkla-Süzgün, Derya Özsavcı, Özlem Bingöl-Özakpınar, Pınar Mega-Tiber, Oya Orun, Pınar Erzincan, Safiye Sağ-Erdem and Fikrettin Şahin

    Article first published online: 19 AUG 2015 | DOI: 10.1002/ardp.201500178

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    The tolmetin hydrazone N′-[(2,6-dichlorophenyl)methylidene]-2-[1-methyl-5-(4-methylbenzoyl)-1H-pyrrol-2-yl]acetohydrazide (4g) exhibited anticancer activity with an IC50 value of 76 µM against HT-29 cells and did not display cytotoxicity toward control fibroblast cells, compared to tolmetin. The anti-cancer activity of 4g was shown to be due to the activation of caspase-8 and caspase-9 involved in apoptosis.

  3. Synthesis, Biological, and Computational Evaluation of Novel 1,3,5-Substituted Indolin-2-One Derivatives as Inhibitors of Src Tyrosine Kinase

    Zühal Kilic-Kurt, Filiz Bakar and Süreyya Ölgen

    Article first published online: 11 AUG 2015 | DOI: 10.1002/ardp.201500109

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    A novel series of indole-2-one derivatives were synthesized and evaluated for their Src inhibitory activities. Compound 2f was found as the most promising compound with an IC50 value of 1.02 µM. Molecular docking studies were performed to disclose the binding mode for compound 2f.

  4. Synthesis and Analgesic Activity of Annelated Xanthine Derivatives in Experimental Models in Rodents

    Małgorzata Zygmunt, Jacek Sapa, Anna Drabczyńska, Tadeusz Karcz, Christa Müller, Meryem Köse, Gniewomir Latacz, Jakub Schabikowski, Marek Bednarski and Katarzyna Kieć-Kononowicz

    Article first published online: 6 AUG 2015 | DOI: 10.1002/ardp.201500169

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    Tetrahydropyrimido[2,1-f]purinediones were synthesized and assayed in the writhing and hot plate tests as potential analgesic agents. 9-Phenethyl-1,3-dipropyl-6,7,8,9-tetrahydropyrimido[1,2-a]purine-2,4(1H,3H)-dione (KD-142) showed the strongest antinociceptive activity (ED50 = 9.0 mg/kg) in the writhing test and the strongest affinity for A2B receptors (Ki = 0.59 μM).

  5. Synthesis and Evaluation of a Series of Oleanolic Acid Saponins as α-Glucosidase and α-Amylase Inhibitors

    Tiantian Guo, Shaoping Wu, Sen Guo, Lu Bai, Qingchao Liu and Naisheng Bai

    Article first published online: 24 JUL 2015 | DOI: 10.1002/ardp.201500179

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    A series of naturally occurring oleanane-type triterpenoid saponins and non-natural oleanolic acid saponins were synthesized, and their inhibitory activities against α-glucosidase and α-amylase were evaluated in vitro. With an IC50 value of 87.3 μM, 28-O-monoglucoside 8 exhibited fivefold stronger inhibitory activity against α-glucosidase than the antidiabetic acarbose.