Discovery and biological evaluation of 2-((3-phenylisoxazol-5-yl) methoxy) benzamide derivatives as potent nucleocapsid inhibitors

被引：4

作者：

Xie, Ziyue ^{[1
]}

Liang, Zhengcheng ^{[1
]}

Huang, Yunhou ^{[1
]}

Shi, Kaichuang ^{[3
]}

Zang, Ning ^{[4
]}

Wang, Mian ^{[2
]}

Liang, Taoyuan ^{[1
]}

Wei, Wanxing ^{[1
]}

机构：

[1] Guangxi Univ, Coll Chem & Chem Engn, Nanning 530004, Peoples R China

[2] Guangxi Univ, Coll Life Sci, Nanning 530004, Peoples R China

[3] Guangxi Ctr Anim Dis Control & Prevent, Nanning 530001, Peoples R China

[4] Guangxi Med Univ, Sch Basic Med, Nanning 530021, Peoples R China

来源：

JOURNAL OF MOLECULAR STRUCTURE | 2023年 / 1272卷

基金：

中国国家自然科学基金;

关键词：

Synthesis; Anti-HBV activity; Biological evaluation; Structure -activity relationships; Molecular docking; MOLECULAR DOCKING; DESIGN; REPLICATION;

D O I：

10.1016/j.molstruc.2022.134103

中图分类号：

O64 [物理化学（理论化学）、化学物理学];

学科分类号：

070304 ; 081704 ;

摘要：

A series of 2-((3-phenylisoxazol-5-yl) methoxy) benzamides derivatives were designed and synthesized, and their anti-hepatitis B virus (HBV) activities were evaluated with HepG2.2.15 cells. The results showed that compounds 10a, 10c, 10d and 10f strongly inhibited secretion of HBeAg (IC50 = 0.20, 0.07, 0.30 and 0.12 mu M, respectively, 3TC in 119.87 mu M). Compounds 8a, 8b, 10c, 10f effectively inhibited HBV DNA replication with IC50 in 7.61, 8.92, 0.10 and 1.49 mu M, respectively and were more effective than 3TC (IC50(DNA) = 13.02 mu M). Result of docking studies indicated that compounds interacted to HBV core protein and coincided to their inhibitions on HBV. This work provided new compounds with significant inhibition on HBV for further optimization and development as potential non-nucleoside anti-virus agents. Mean-while, chlorination on phenyl ring of dimethoxybenzaldehyde oxime occurred and did not follow Friedel -Crafts substitution when the oxime reacted with excess NCS.(c) 2022 Elsevier B.V. All rights reserved.

引用

页数：11

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