鉴定1-异丙基磺酰基-2-胺基苯并咪唑为一类新型乙型肝炎病毒抑制剂。
Identification of 1-isopropylsulfonyl-2-amine benzimidazoles as a new class of inhibitors of hepatitis B virus.
作者信息
Li Yun-Fei, Wang Gui-Feng, Luo Yu, Huang Wei-Gang, Tang Wei, Feng Chun-Lan, Shi Li-Ping, Ren Yu-Dan, Zuo Jian-Ping, Lu Wei
机构信息
Institute of Medicinal Chemistry, Shanghai Key Laboratory of Green Chemistry and Chemical Process, Department of Chemistry, East China Normal University, 3663 North Zhongshan Road, Shanghai, Shanghai 200062, China.
出版信息
Eur J Med Chem. 2007 Nov-Dec;42(11-12):1358-64. doi: 10.1016/j.ejmech.2007.03.005. Epub 2007 Mar 31.
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 (IC(50)<4 microM) with high selectivity indices (SIs>40). Compounds 5b-e, g, j, and 9a were among the most prominent compounds, with IC(50)s of 0.70-2.0 microM and SIs of 41-274. The potent anti-HBV activity and safety profiles of the most promising compounds 5d and j (IC(50)s=0.70 microM, SIs>120) demonstrate the potential of this series of benzimidazoles for the development of new anti-HBV drugs.
合成了一系列1-异丙基磺酰基-2-胺苯并咪唑衍生物，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。总体而言，这些衍生物是强效的HBV抑制剂（IC(50)<4 microM），具有高选择性指数（SIs>40）。化合物5b-e、g、j和9a是最突出的化合物，IC(50)为0.70-2.0 microM，SIs为41-274。最有前景的化合物5d和j（IC(50)=0.70 microM，SIs>120）的强效抗HBV活性和安全性表明了该系列苯并咪唑在开发新型抗HBV药物方面的潜力。
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