Synthesis of novel substituted N-aryl benzamides as hA3G stabilizers and their inhibitory activities against hepatitis C virus replication  

作　　者：Yanping Li Zonggen Peng Lanhu Hao Zhouyi Wu Yanping Zhu Laixing Hu Jiandong Jiang Zhuorong Li 

机构地区：[1]Institute of Medicinal Biotechnology,Chinese Academy of Medical Sciences&Peking Union Medical College,Beijing 100050,China

出　　处：《Acta Pharmaceutica Sinica B》2013年第5期312-321,共10页药学学报（英文版）

基　　金：supported by the National Natural Science Foundation of China(Grants 30873138,81202414).

摘　　要：A series of novel amino-substituted N-aryl benzamide analogs were synthesized and evaluated for their ability to inhibit hepatitis C virus(HCV)replication in acutely infected Huh7.5 cells.Most of the substituted N-aryl benzamide compounds showed convincing anti-HCV activities.Compounds 1f,1g and 4c exhibited potent anti-replicative activity at low micromolar levels(IC_(50)=1.0–2.0μM)with selective indices(SI)greater than 40.Mechanistic analysis indicated that the active compounds increased intracellular hA3G protein levels and inhibited HCV replication in a dose-dependent manner.The results demonstrate that this series of substituted Naryl benzamide compounds warrant further investigation as inhibitors of HCV replication.

关 键 词：N-aryl benzamide hA3G HCV inhibitor Structure–activity relationship 

分 类 号：O62[理学—有机化学]