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

…, S Baumeister, PE Wiedeman, L Traphagen…

Index: 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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Citation Number: 19

Abstract

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 ...