2. Academic Validation
  3. Synthesis and biological evaluation of 1H-benzimidazol-5-ols as potent HBV inhibitors

Synthesis and biological evaluation of 1H-benzimidazol-5-ols as potent HBV inhibitors

  • Bioorg Med Chem Lett. 2010 Dec 15;20(24):7230-3. doi: 10.1016/j.bmcl.2010.10.099.
Yanfang Zhao 1,  Yajing Liu,  Dong Chen,  Zengquan Wei,  Wenzhao Liu,  Ping Gong
Affiliations

Affiliation

  • 1 Key Lab of Structure-Based Drug Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, PR China.
PMID: 21074429 DOI: 10.1016/j.bmcl.2010.10.099
Abstract

A new series of 1-methyl-1H-benzimidazol-5-ol derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. Some of the analogues in this series displayed inhibitory activity superior to lamivudine. Of them, compound 13b was the most potent one, showing an IC(50) value of 7.8 μM and a SI value of 13.0.

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