Synthesis of novel substituted N-aryl benzamides as hA3G stabilizers and their inhibitory activities against hepatitis C virus replication
| Autor: | Yanping Li, Zonggen Peng, Lanhu Hao, Zhouyi Wu, Yanping Zhu, Laixing Hu, Jiandong Jiang, Zhuorong Li |
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| Jazyk: | angličtina |
| Rok vydání: | 2013 |
| Předmět: | |
| Zdroj: | Acta Pharmaceutica Sinica B, Vol 3, Iss 5, Pp 312-321 (2013) |
| Druh dokumentu: | article |
| ISSN: | 2211-3835 2211-3843 |
| DOI: | 10.1016/j.apsb.2013.07.002 |
| Popis: | 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 (IC50=1.0–2.0 μM) 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 N-aryl benzamide compounds warrant further investigation as inhibitors of HCV replication. |
| Databáze: | Directory of Open Access Journals |
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