2,4-Diaryl-4,6,7,8-tetrahydroquinazolin-5(1H)-one derivatives as anti-HBV agents targeting at capsid assembly

被引：65

作者：

Zhu, Xuejun ^{[1
,2
]}

Zhao, Guoming ^{[2
]}

Zhou, Xiaoping ^{[1
]}

Xu, Xiaoqian ^{[2
,3
]}

Xia, Guangqiang ^{[2
]}

Zheng, Zhibing ^{[2
]}

Wang, Lili ^{[2
]}

Yang, Xiaohong ^{[1
]}

Li, Song ^{[2
]}

机构：

[1] Jilin Univ, Sch Pharm, Changchun 130021, Peoples R China

[2] Beijing Inst Pharmacol & Toxicol, Dept Med Chem, Beijing 100850, Peoples R China

[3] Shenyang Pharmaceut Univ, Sch Pharmaceut Engn, Shenyang 110016, Peoples R China

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 01期

关键词：

2,4-Diaryl-4,6,7,8-tetrahydroquinazolin-5(1H)-one; Hepatitis B virus (HBV); Nucleocapsid assembly; Inhibitor; B-VIRUS-REPLICATION; CHRONIC HEPATITIS-B; PROTEIN; INHIBITION; MODEL;

D O I：

10.1016/j.bmcl.2009.10.119

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 2,4-diaryl-4,6,7,8-tetrahydroquinazolin-5(1H)-one derivatives were designed and synthesized as potent inhibitors of HBV capsid assembly. These compounds arose from efforts to rigidify an earlier series of heteroaryldihydropyrimidines (HAPs), and compounds 12, 13, 20, 24, 30 and 32 showed potent inhibition of HBV capsid assembly, especially 24 with IC50 value at sub-micromolar range. (c) 2009 Elsevier Ltd. All rights reserved.

引用

页码：299 / 301

页数：3

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