2. Academic Validation
  3. Design and synthesis of novel benzimidazole derivatives as inhibitors of hepatitis B virus

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

  • Bioorg Med Chem. 2010 Jul 15;18(14):5048-55. doi: 10.1016/j.bmc.2010.05.076.
Yu Luo 1,  Jia-Ping Yao,  Li Yang,  Chun-Lan Feng,  Wei Tang,  Gui-Feng Wang,  Jian-Pin Zuo,  Wei Lu
Affiliations

Affiliation

  • 1 Department of Chemistry, East China Normal University, 3663 North Zhongshan Road, Shanghai 200062, PR China.
PMID: 20639110 DOI: 10.1016/j.bmc.2010.05.076
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.

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