Identification of halosalicylamide derivatives as a novel class of allosteric inhibitors of HCV NS5B polymerase

…, S Baumeister, PE Wiedeman, L Traphagen…

文献索引：Liu, Yaya; Donner, Pamela L.; Pratt, John K.; Jiang, Wen W.; Ng, Teresa; Gracias, Vijaya; Baumeister, Steve; Wiedeman, Paul E.; Traphagen, Linda; Warrior, Usha; Maring, Clarence; Kati, Warren M.; Djuric, Stevan W.; Molla, Akhteruzzaman Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 11 p. 3173 - 3177

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被引用次数: 19

摘要

Halosalicylamide derivatives were identified from high-throughput screening as potent inhibitors of HCV NS5B polymerase. The subsequent structure and activity relationship revealed the absolute requirement of the salicylamide moiety for optimum activity. Methylation of either the hydroxyl group or the amide group of the salicylamide moiety abolished the activity while the substitutions on both phenyl rings are acceptable. The ...