Archiv der Pharmazie

Cover image for Vol. 348 Issue 7

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. Design, Synthesis, and Biological Evaluation of Dabigatran Etexilate Mimics, a Novel Class of Thrombin Inhibitors

    Shaochi Wang, Peng Dai, Yungen Xu, Qiufang Chen, Qihua Zhu and Guoqing Gong

    Article first published online: 29 JUN 2015 | DOI: 10.1002/ardp.201500101

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    After scaffold hopping, the novel dabigatran etexilate analogues possess moderate inhibitory activity toward platelet aggregation induced by thrombin in vitro. The bifunctional prodrug I-8 ((3,5,6-trimethylpyrazin-2-yl)methyl.3-(2-(4-(N′-((hexyloxy)carbonyl)carbamimidoyl)benzyl)-N-(pyridin-2-yl)-1,2,3,4-tetrahydrobenzo[4,5]imidazo[1,2-a]pyrazine-8-carboxamido)propanoate) shows good antithrombotic effects in vitro (IC50 = 9.74 ± 0.94 μM) and in vivo.

  2. Synthesis and Characterization of New 1,2,4-Triazolo[1,5-a]pyridines That Extend the Life Span of Caenorhabiditis elegans via Their Anti-Inflammatory/Antioxidant Effects

    Ramadan A. Mekheimer, Ahmed A. Radwan Sayed, Eltaib A. Ahmed and Kamal U. Sadek

    Article first published online: 18 JUN 2015 | DOI: 10.1002/ardp.201500069

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    A new set of 1,2,4-triazolo[1,5-a]pyridines and their fused ring systems were synthesized and assayed for their anti-inflammatory and antioxidative activities. In the model system Caenorhabiditis elegans, the compounds led to increased heat stress resistance, reduced the formation of advanced glycation end-products, and also extended the life span of the model organism.

  3. The Mechanism of the Interactions of Pironetin Analog/Combretastatin A-4 Hybrids with Tubulin

    Sandra Torijano-Gutiérrez, Concepción Vilanova, Santiago Díaz-Oltra, Juan Murga, Eva Falomir, Miguel Carda, Mariano Redondo-Horcajo, José Fernando Díaz, Isabel Barasoain and Juan Alberto Marco

    Article first published online: 17 JUN 2015 | DOI: 10.1002/ardp.201500106

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    The interactions with tubulin of several cytotoxic pironetin analog/combretastatin A-4 hybrids were investigated. Even though the natural products pironetin and combretastatin A-4 are known to interact with tubulin at different sites, only some of the synthetic hybrid molecules show such type of interactions, which are in addition dependent on the length of the spacer fragment.

  4. Synthesis, Antimicrobial, Antiquorum-Sensing, and Cytotoxic Activities of New Series of Isoindoline-1,3-dione, Pyrazolo[5,1-a]isoindole, and Pyridine Derivatives

    Nadia S. El-Gohary and Mona I. Shaaban

    Article first published online: 16 JUN 2015 | DOI: 10.1002/ardp.201500037

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    New series of isoindoline-1,3-diones, pyrazolo[5,1-a]isoindoles, and pyridines were synthesized and screened for their antibacterial, antifungal, and antiquorum-sensing activities. Compound 5, one of the new isoindoline-1,3-diones, is the most active and least cytotoxic member in this study, with broad-spectrum antimicrobial activity.

  5. Synthesis and Anticonvulsant Activity Evaluation of 4-Phenyl-[1,2,4]triazolo[4,3-a]quinazolin-5(4H)-one and Its Derivatives

    Hong-Jian Zhang, Peng Jin, Shi-Ben Wang, Fu-Nan Li, Li-Ping Guan and Zhe-Shan Quan

    Article first published online: 5 JUN 2015 | DOI: 10.1002/ardp.201500115

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    A series of 4-(substituted-phenyl)-[1,2,4]triazolo[4,3-a]quinazolin-5(4H)-ones with triazole and other heterocyclic substituents were synthesized and the compounds were evaluated for their anticonvulsant activity and neurotoxicity using maximal electroshock and rotarod neurotoxicity tests.