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

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• 作者：Xuejun Zhu ; Guoming Zhao ; Xiaoping Zhou ; Xiaoqian Xu ; Guangqiang Xia ; Zhibing Zheng ; Lili Wang ; Xiaohong Yang ; Song Li
• 关键词：2 ; 4-Diaryl-4 ; 6 ; 7 ; 8-tetrahydroquinazolin-5(1H)-one ; Hepatitis B virus (HBV) ; Nucleocapsid assembly ; Inhibitor
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2010
• 出版时间：1 January 2010
• 年：2010
• 卷：20
• 期：1
• 页码：299-301
• 全文大小：217 K

文摘

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.