Archiv der Pharmazie
© WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim
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
|Online Only in 2015|
Archiv der Pharmazie is now online only as of January 2015. All content will be at your fingertips right here on Wiley Online Library.
Recently Published Articles
- 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
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.
- 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
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.
- 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
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.
- 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
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.
- 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
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.