Bioorganic & Medicinal Chemistry 2010-07-15

Design and synthesis of novel benzimidazole derivatives as inhibitors of hepatitis B virus.

Yu Luo, Jia-Ping Yao, Li Yang, Chun-Lan Feng, Wei Tang, Gui-Feng Wang, Jian-Pin Zuo, Wei Lu

Index: Bioorg. Med. Chem. 18(14) , 5048-55, (2010)

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Abstract

A series of novel benzimidazole derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. The preliminary SAR was discussed. Compound 12a, with IC50<0.41 microM and SI>81.2, was the most promising compound and selected as the benchmark compound for further optimization.Copyright (c) 2010 Elsevier Ltd. All rights reserved.