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

Xuejun Zhu; Guoming Zhao; Xiaoping Zhou; Xiaoqian Xu; Guangqiang Xia; Zhibing Zheng; Lili Wang; Xiaohong Yang; Song Li

doi:10.1016/j.bmcl.2009.10.119

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

Bioorg Med Chem Lett. 2010 Jan 1;20(1):299-301. doi: 10.1016/j.bmcl.2009.10.119. Epub 2009 Oct 30.

Authors

Xuejun Zhu¹, Guoming Zhao, Xiaoping Zhou, Xiaoqian Xu, Guangqiang Xia, Zhibing Zheng, Lili Wang, Xiaohong Yang, Song Li

Affiliation

¹ School of Pharmacy, Jilin University, Changchun 130021, PR China.

PMID: 19897363
DOI: 10.1016/j.bmcl.2009.10.119

Abstract

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 IC(50) value at sub-micromolar range.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Antiviral Agents / chemical synthesis
Antiviral Agents / chemistry*
Antiviral Agents / pharmacology
Capsid / drug effects
Capsid / metabolism*
Quinazolinones / chemical synthesis
Quinazolinones / chemistry*
Quinazolinones / pharmacology
Structure-Activity Relationship
Virus Replication / drug effects

Substances

Antiviral Agents
Quinazolinones