Structure–activity relationships of antitubercular salicylanilides consistent with disruption of the proton gradient via proton shuttling

…, A Samuels, M Yun, B Nam, M Kang, K Crowley…

文献索引：Lee, Ill-Young; Gruber, Todd D.; Samuels, Amanda; Yun, Minhan; Nam, Bora; Kang, Minseo; Crowley, Kathryn; Winterroth, Benjamin; Boshoff, Helena I.; Barry III, Clifton E. Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 1 p. 114 - 126

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被引用次数: 15

摘要

A series of salicylanilides was synthesized based on a high-throughput screening hit against Mycobacterium tuberculosis. A free phenolic hydroxyl on the salicylic acid moeity is required for activity, and the structure–activity relationship of the aniline ring is largely driven by the presence of electron withdrawing groups. We synthesized 94 analogs exploring substitutions of both rings and the linker region in this series and we have identified ...