Design, Synthesis and Biological Activity of Novel Chalcone Derivatives as Anti-influenza Agents

doi:10.1007/s40242-015-5356-z

高等学校化学研究 ›› 2016, Vol. 32 ›› Issue (1): 28-34.doi: 10.1007/s40242-015-5356-z

Design, Synthesis and Biological Activity of Novel Chalcone Derivatives as Anti-influenza Agents

SHI Fangyuan, FANG Hao, XU Wenfang

Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan 250012, P. R. China

收稿日期:2015-09-14 修回日期:2015-11-13 出版日期:2016-02-01 发布日期:2015-11-30
通讯作者: XU Wenfang E-mail:wenfxu@163.com
基金资助:
Supported by the National High-tech R&D Program of China(No.2014AA020523), the National Natural Science Foundation of China(Nos.21302111, 81373282, 21172134) and the China Postdoctoral Science Foundation Funded Project (Nos.2013M540558, 2014T70654).

Design, Synthesis and Biological Activity of Novel Chalcone Derivatives as Anti-influenza Agents

SHI Fangyuan, FANG Hao, XU Wenfang

Department of Medicinal Chemistry, School of Pharmaceutical Sciences, Shandong University, Jinan 250012, P. R. China

Received:2015-09-14 Revised:2015-11-13 Online:2016-02-01 Published:2015-11-30
Contact: XU Wenfang E-mail:wenfxu@163.com
Supported by:
Supported by the National High-tech R&D Program of China(No.2014AA020523), the National Natural Science Foundation of China(Nos.21302111, 81373282, 21172134) and the China Postdoctoral Science Foundation Funded Project (Nos.2013M540558, 2014T70654).

摘要/Abstract

摘要：

A series of novel chalcone derivatives was designed and synthesized via a suitable synthetic strategy in good yields using commercially available 2-amino-4-nitrophenol as an initiator. The structures of the target compounds were confirmed by means of ¹H NMR, ¹³C NMR and high-resolution mass spectrometry(HRMS). And the ability of the target compounds to inhibit influenza viruses was evaluated. These compounds showed moderate inhibitory activity against influenza A(H9N2 and H5N1) viruses. Within this series, compounds S14 and S15 with good potency(IC₅₀=40.3-51.5μmol/L) could be used as lead compounds in the future.

关键词: Influenza virus, Inhibitor, Chalcone, Biological activity

Abstract:

Key words: Influenza virus, Inhibitor, Chalcone, Biological activity

SHI Fangyuan, FANG Hao, XU Wenfang. Design, Synthesis and Biological Activity of Novel Chalcone Derivatives as Anti-influenza Agents[J]. 高等学校化学研究, 2016, 32(1): 28-34.

SHI Fangyuan, FANG Hao, XU Wenfang. Design, Synthesis and Biological Activity of Novel Chalcone Derivatives as Anti-influenza Agents[J]. Chemical Research in Chinese Universities, 2016, 32(1): 28-34.

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Design, Synthesis and Biological Activity of Novel Chalcone Derivatives as Anti-influenza Agents

Design, Synthesis and Biological Activity of Novel Chalcone Derivatives as Anti-influenza Agents

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