Synthesis and anti-hepatitis B virus activity of novel benzimidazole derivatives

J Med Chem. 2006 Jul 27;49(15):4790-4. doi: 10.1021/jm060330f.

Yun-Fei Li ¹, Gui-Feng Wang, Pei-Lan He, Wei-Gang Huang, Feng-Hua Zhu, He-Yong Gao, Wei Tang, Yu Luo, Chun-Lan Feng, Li-Ping Shi, Yu-Dan Ren, Wei Lu, Jian-Ping Zuo

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Affiliation

1 State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, SIBS, Chinese Academy of Sciences, 555 Zuchongzhi Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China.

PMID: 16854087 DOI: 10.1021/jm060330f

Abstract

A series of novel benzimidazole derivatives was synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in vitro. Strong activity against HBV replication and low cytotoxicity were generally observed in these benzimidazoles. The most promising compounds were 12a and 12b, with similar high Antiviral potency (IC50 = 0.9 and 0.7 microM, respectively) and remarkable selectivity indices (>1111 and 714, respectively). They were selected for further evaluation as novel HBV inhibitors.

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