کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1398177 | 1501218 | 2007 | 7 صفحه PDF | دانلود رایگان |
A series of 1-isopropylsulfonyl-2-amine benzimidazole derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in the HepG2.2.15 cell line. In general, these derivatives are potent HBV inhibitors (IC50 < 4 μM) with high selectivity indices (SIs > 40). Compounds 5b–e, g, j, and 9a were among the most prominent compounds, with IC50s of 0.70–2.0 μM and SIs of 41–274. The potent anti-HBV activity and safety profiles of the most promising compounds 5d and j (IC50s = 0.70 μM, SIs > 120) demonstrate the potential of this series of benzimidazoles for the development of new anti-HBV drugs.
Synthesis of a series of 1-isopropylsulfonyl-2-amine benzimidazoles and their significant inhibitory activities against hepatitis B virus in vitro is presented.Figure optionsDownload as PowerPoint slide
Journal: European Journal of Medicinal Chemistry - Volume 42, Issues 11–12, November–December 2007, Pages 1358–1364