Archiv der Pharmazie

Cover image for Vol. 348 Issue 1

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. Susceptibility of Candida albicans to New Synthetic Sulfone Derivatives

    Monika Staniszewska, Małgorzata Bondaryk and Zbigniew Ochal

    Article first published online: 14 JAN 2015 | DOI: 10.1002/ardp.201400360

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    The influence of halogenated methyl sulfones on cell growth inhibition, aspartic protease gene expression, adhesion to epithelium, and filamentation was investigated. Halogenated methyl sulfones containing bromodichloromethyl or dichloromethyl at C-4 of the phenyl ring showed the best activity, while hydrazine at C-1 reduced the sulfone potential. The halogenated methyl sulfones were shown to inhibit biofilm formation by interfering with adherence and the yeast-to-hyphae transition of Candida albicans.

  2. Novel Mcl-1/Bcl-2 Dual Inhibitors Created by the Structure-Based Hybridization of Drug-Divided Building Blocks and a Fragment Deconstructed from a Known Two-Face BH3 Mimetic

    Zhichao Zhang, Pengchen Su, Xiangqian Li, Ting Song, Gaobo Chai, Xiaoyan Yu and Keren Zhang

    Article first published online: 13 JAN 2015 | DOI: 10.1002/ardp.201400296

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    2-Phenyl-1H-benzo[d]imidazole was developed as a new scaffold for two-face Bim mimetics, resulting in a series of Mcl-1/Bcl-2 dual inhibitors. The most potent compound binds to Mcl-1 and Bcl-2 with Ki values of 127 and 607 nM, respectively, and induces apoptosis in multiple cancer cell lines.

  3. Design, Synthesis, Biological Evaluation and Binding Mode Modeling of Benzimidazole Derivatives Targeting the Cannabinoid Receptor Type 1

    Christian Espinosa-Bustos, Carlos F. Lagos, Javier Romero-Parra, Ana M. Zárate, Jaime Mella-Raipán, Hernán Pessoa-Mahana, Gonzalo Recabarren-Gajardo, Patricio Iturriaga-Vásquez, Ricardo A. Tapia and C. David Pessoa-Mahana

    Article first published online: 13 JAN 2015 | DOI: 10.1002/ardp.201400201

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    Novel N-acyl-2,5-dimethoxyphenyl-1H-benzimidazoles were designed based on a CoMFA model for cannabinoid receptor type 1 (CB1) ligands. The most promising derivative (5) displayed a Ki value of 1.2 nM when compared to CP55,940. New information is provided for the development of small molecules with high CB1 affinity.

  4. You have free access to this content
    Next Steps in Advancing Publication (page 1)

    Holger Stark

    Article first published online: 8 JAN 2015 | DOI: 10.1002/ardp.201570004

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    Piperazine Analogs of Naphthyridine-3-carboxamides and Indole-2-carboxamides: Novel 5-HT3 Receptor Antagonists with Antidepressant-Like Activity (pages 34–45)

    Arghya K. Dhar, Radhakrishnan Mahesh, Ankur Jindal and Shvetank Bhatt

    Article first published online: 8 JAN 2015 | DOI: 10.1002/ardp.201400293

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    Piperazine analogs of naphthyridine-3-carboxamides and indole-2-carboxamides were designed using a ligand-based approach, according to the pharmacophoric requirements for 5-HT3 receptor antagonists. The piperazine derivatives of indole-2-carboxamide 13i and naphthyridine-3-carboxamide 8h exhibited prominent 5-HT3 receptor antagonism with pA2 values of 7.5 and 7.3, respectively. Compounds 8h and 13i also showed the most promising antidepressant activities.

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