Chemical Biology & Drug Design

Cover image for Vol. 85 Issue 3

Edited By: David Selwood

Impact Factor: 2.507

ISI Journal Citation Reports © Ranking: 2013: 28/58 (Chemistry Medicinal); 173/291 (Biochemistry & Molecular Biology)

Online ISSN: 1747-0285

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Editor's Choice

Synthesis and Biological Evaluation of 2-oxo-pyrazine-3-carboxamide-yl Nucleoside Analogues and Their Epimers as Inhibitors of Influenza A Viruses

Jingjing Gao, Xianjin Luo, Yuhuan Li, Rongmei Gao, Haifeng Chen and Dingjue Ji

Graphical Abstract-Scheme

Novel 2-oxo-pyrazine-3-carboxamide-yl nucleoside analogues and their epimers were designed, synthesized, and evaluated for their activities against influenza A viruses H1N1 and H3N2 in MDCK cells. All the compounds showed low cytotoxicities in these anti-influenza tests. One of the epimers 8a shows high antiviral activity (IC50 = 7.41, 5.63 μm for H3N2 and H1N1, respectively) and remarkable low cytotoxicity (TC50 > 200 μm). Molecular docking of compound 8a with RNA-dependent RNA polymerase was performed to understand the binding mode between these inhibitors and the active site of RdRp.

This issue’s Editor’s Choice was chosen by Masahiro Okuyama

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We are pleased to announce that a member of our Editorial Board, Jurgen Bajorath, has won the 2015 Skolnik Award for his outstanding contributions to information science.

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