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Synthesis and in vitro anti-hepatitis B virus activity of 1H-benzimidazol-5-ol derivatives
Authors:Dong Chen  Xin Zhai  Qiu Hui Yuan  Jian Luo  Si Chang Xie  Ping Gong
Institution:Key Laboratory of Original New Drugs Design and Discovery of Ministry of Education;School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China
Abstract:A series of 1H-benzimidazol-5-ol derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in HepG2.2.15 cells. Half of the tested compounds were found to be potent against HBsAg secretion with IC50 values less than 100 μmol/L. Compounds 14c, 14d, and 14e showed significant inhibitory activity to the viral antigen HBeAg.
Keywords:1H-Benzimidazol-5-ol  Synthesis  Anti-HBV activity
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