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Synthesis and anti-hepatitis B virus activity of novel benzimidazole derivatives

机译:新型苯并咪唑衍生物的合成及其抗乙肝病毒活性

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摘要

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 AM, respectively) and remarkable selectivity indices (> 1111 and 714, respectively). They were selected for further evaluation as novel HBV inhibitors.
机译: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。在这些苯并咪唑中通常观察到抗HBV复制的强活性和低细胞毒性。最有前途的化合物是12a和12b,具有相似的高抗病毒效力(分别为IC50 = 0.9和0.7 AM)和显着的选择性指数(分别为> 1111和714)。选择它们作为新的HBV抑制剂进行进一步评估。

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