Synthesis and evaluation of steroidal thiazoline conjugates as potential antiviral agents

文献类型： 外文期刊

第一作者： Ke, Shaoyong

作者： Ke, Shaoyong;Shi, Liqiao;Zhang, Zhigang;Fang, Wei;Zhang, Ya-Ni;Wang, Kaimei;Zhou, Ronghua;Wan, Zhongyi;Yang, Ziwen;Zhang, Guangyang;Li, Ni;Wei, Yanhong;Ke, Ting;Ke, Shaoyong

作者机构：

关键词： antiviral activity; coxsackie virus type B; dehydroepiandrosterone; enterovirus 71; steroid; thiazoline

期刊名称：FUTURE MEDICINAL CHEMISTRY （ 影响因子：3.808； 五年影响因子：4.604 ）

ISSN： 1756-8919

年卷期： 2018 年 10 卷 22 期

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收录情况： SCI

摘要： Aim: Many heterocyclic compounds derived from natural steroids exhibited broad activities, so this work focused on the investigations on a series of steroidal thiazoline conjugates as antiviral agents. Materials & methods:A series of steroid derivatives containing thiazoline heterocycles were designed and synthesized via a convenient condensation procedure. The compounds were screened for their potential antivirus activities against Enterovirus 71 (EV71) and Coxsackie Virus Type B (CVB3). Results and Conclusion: The in vitro bioassay indicated that compounds 5b, 5g and 5i exhibited excellent antiviral effects on EV71, and compounds 5b, 5e, 6c and 6g presented better antiviral activities against CVB3 compared with the controls ribavirin or pirodavir. These results indicate that these steroidal thiazoline conjugates might be feasible therapeutic candidates against EV71 infection, which might also be considered as promising compounds for optimization of potential antivirus agents.

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