Design, synthesis, and antiviral activities of 1,5-benzothiazepine derivatives containing pyridine moiety

被引：51

作者：

Li, Tianxian ^{[1
]}

Zhang, Jian ^{[1
]}

Pan, Jianke ^{[1
]}

Wu, Zengxue ^{[1
]}

Hu, Deyu ^{[1
]}

Song, Baoan ^{[1
]}

机构：

[1] Guizhou Univ, State Key Lab Breeding Base Green Pesticide & Agr, Key Lab Green Pesticide & Agr Bioengn, Minist Educ, Guiyang 550025, Peoples R China

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2017年 / 125卷

基金：

中国国家自然科学基金;

关键词：

Benzothiazepine derivatives; Pyridine; 1,3-Dipolar cycloaddition; Antiviral activity; BIOLOGICAL EVALUATION; ANTICANCER; INHIBITORS; ANALOGS; VIRUS;

D O I：

10.1016/j.ejmech.2016.09.069

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

In our previous work, a series of novel benzothiazepine derivatives containing pyridine moiety were successfully synthesized through chalcone 1,3-dipolar cycloaddition and determined their antiviral activity against tobacco mosaic virus (TMV). Bioassay results indicated that most of these target compounds exhibited improved curative, protection, and inactivation activity in vivo than the commercial agent ningnanmycin. Particularly, compound 3m exhibited marked curative activity against TMV, with an EC50 value of 352.2 mu M, which was even better than that of ningnanmycin. The compound was identified as the most promising candidate for inhibiting plant virus and an excellent compound with antiviral activities against TMV. Structure activity relationship experiment indicated that the 1,5-benzothiazepine moiety is crucial for potent anti-TMV activity. (C) 2016 Elsevier Masson SAS. All rights reserved.

引用

页码：657 / 662

页数：6

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