新型苯并咪唑衍生物的合成及其抗乙型肝炎病毒活性
Synthesis and anti-hepatitis B virus activity of novel benzimidazole derivatives.
作者信息
Li Yun-Fei, Wang Gui-Feng, He Pei-Lan, Huang Wei-Gang, Zhu Feng-Hua, Gao He-Yong, Tang Wei, Luo Yu, Feng Chun-Lan, Shi Li-Ping, Ren Yu-Dan, Lu Wei, Zuo Jian-Ping
机构信息
State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, SIBS, Chinese Academy of Sciences, 555 Zuchongzhi Road, Zhangjiang Hi-Tech Park, Shanghai 201203, China.
出版信息
J Med Chem. 2006 Jul 27;49(15):4790-4. doi: 10.1021/jm060330f.
A series of novel benzimidazole derivatives was synthesized and evaluated for their anti-hepatitis B virus (HBV) activity and cytotoxicity in vitro. Strong activity against HBV replication and low cytotoxicity were generally observed in these benzimidazoles. The most promising compounds were 12a and 12b, with similar high antiviral potency (IC50 = 0.9 and 0.7 microM, respectively) and remarkable selectivity indices (>1111 and 714, respectively). They were selected for further evaluation as novel HBV inhibitors.
合成了一系列新型苯并咪唑衍生物，并对其体外抗乙型肝炎病毒（HBV）活性和细胞毒性进行了评估。在这些苯并咪唑中普遍观察到对HBV复制有较强活性且细胞毒性较低。最有前景的化合物是12a和12b，具有相似的高抗病毒效力（IC50分别为0.9和0.7微摩尔）和显著的选择性指数（分别>1111和714）。它们被选作新型HBV抑制剂进行进一步评估。
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