Archiv der Pharmazie
Copyright © 2014 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
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
|Online Only in 2015|
Archiv der Pharmazie will be online only as of January 2015. All content will be at your fingertips right here on Wiley Online Library.
Recently Published Articles
- 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
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.
- 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
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.
- 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
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.
- You have free access to this content
- You have free access to this contentPiperazine 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
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.