2,4-Diaryl-4,6,7,8-tetrahydroquinazolin-5(1H)-one derivatives as anti-HBV agents targeting at capsid assembly.
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.
Zhu
Xuejun
X
School of Pharmacy, Jilin University, Changchun 130021, PR China.
Zhao
Guoming
G
Zhou
Xiaoping
X
Xu
Xiaoqian
X
Xia
Guangqiang
G
Zheng
Zhibing
Z
Wang
Lili
L
Yang
Xiaohong
X
Li
Song
S
D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D002213:Capsid / Q000187:drug effects / Q000378:metabolism*; D052999:Quinazolinones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014779:Virus Replication / Q000187:drug effects
D000998:Antiviral Agents; D052999:Quinazolinones