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

• Published in: Chemical research in Chinese universities Vol. 32; no. 1; pp. 28 - 34
• Main Authors: Shi, Fangyuan, Fang, Hao, Xu, Wenfang
• Format: Journal Article
• Language: English
• Published: Changchun Jilin University and The Editorial Department of Chemical Research in Chinese Universities 01-02-2016
• Subjects: 4-硝基酚; Analytical Chemistry; Chemistry; Chemistry and Materials Science; Chemistry/Food Science; Inorganic Chemistry; Organic Chemistry; Physical Chemistry; 抗流感病毒; 查尔酮衍生物; 生物活性; 药物; 设计; 铅化合物; 高分辨质谱; Inhibitor; Influenza virus; Chalcone; Biological activity
• ISSN: 1005-9040; 2210-3171
• DOI: 10.1007/s40242-015-5356-z

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 IH 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 inhi- bitory activity against influenza A（H9N2 and H5NI） viruses. Within this series, compounds S14 and S15 with good potency（IC50=40.3--51.5 μmol/L） could be used as lead compounds in the future.