Synthesis and Anti-Hepatitis B Virus Activity of a Novel Class of Thiazolylbenzimidazole Derivatives

被引：20

作者：

Luo, Yu ^{[1
]}

Yao, Jia-Ping ^{[1
]}

Yang, Li ^{[2
]}

Feng, Chun-Lan ^{[2
]}

Tang, Wei ^{[2
]}

Wang, Gui-Feng ^{[2
]}

Zuo, Jian-Pin ^{[2
]}

Lu, Wei ^{[1
,3
]}

机构：

[1] E China Normal Univ, Dept Chem, Shanghai 200062, Peoples R China

[2] Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai, Peoples R China

[3] E China Normal Univ, Inst Drug Discovery & Dev, Shanghai 200062, Peoples R China

来源：

ARCHIV DER PHARMAZIE | 2011年 / 344卷 / 02期

关键词：

Anti-HBV; Synthesis; Thiazolylbenzimidazole; BENZIMIDAZOLE DERIVATIVES; NS5B POLYMERASE; IN-VITRO; INHIBITORS; IDENTIFICATION; REPLICATION; DESIGN; ACIDS; VIVO;

D O I：

10.1002/ardp.201000167

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Recently, heterocyclic benzimidazole derivatives have been investigated and validated as a promising class of antiviral agents. In this paper, a series of novel thiazolylbenzimidazole derivatives was synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity on the HepG2.2.15 cell line. Afterwards, the preliminary structure-activity relationship (SAR) was discussed. Compound 8b, with IC(50) 1.1 mu M and SI > 90.9, was the most promising compound and could be selected as a benchmark compound for further investigation.

引用

页码：78 / 83

页数：6

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