Structure–activity relationships of 2-aminothiazoles effective against Mycobacterium tuberculosis

A Meissner, HI Boshoff, M Vasan, BP Duckworth…

文献索引：Meissner, Anja; Boshoff, Helena I.; Vasan, Mahalakshmi; Duckworth, Benjamin P.; Barry III, Clifton E.; Aldrich, Courtney C. Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 21 p. 6385 - 6397

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被引用次数: 16

摘要

Abstract A series of 2-aminothiazoles was synthesized based on a HTS scaffold from a whole-cell screen against Mycobacterium tuberculosis (Mtb). The SAR shows the central thiazole moiety and the 2-pyridyl moiety at C-4 of the thiazole are intolerant to modification. However, the N-2 position of the aminothiazole exhibits high flexibility and we successfully improved the antitubercular activity of the initial hit by more than 128-fold through ...