合成并评价 1H-苯并咪唑-5-醇类化合物作为有效的 HBV 抑制剂。
Synthesis and biological evaluation of 1H-benzimidazol-5-ols as potent HBV inhibitors.
机构信息
Key Lab of Structure-Based Drug Design & Discovery of Ministry of Education, School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, PR China.
出版信息
Bioorg Med Chem Lett. 2010 Dec 15;20(24):7230-3. doi: 10.1016/j.bmcl.2010.10.099. Epub 2010 Oct 26.
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.
合成了一系列新的 1-甲基-1H-苯并咪唑-5-醇衍生物，并在 HepG2.2.15 细胞系中评估了它们的抗乙型肝炎病毒 (HBV) 活性和细胞毒性。该系列中的一些类似物表现出优于拉米夫定的抑制活性。其中，化合物 13b 是最有效的一种，其 IC50值为 7.8 μM，SI 值为 13.0。
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