Synthesis and structure–activity relationships of phenyl-substituted coumarins with anti-tubercular activity that target FadD32

…, N Iwase, M Shimizu, SA Stanley, S Wellington…

Index: Kawate, Tomohiko; Iwase, Noriaki; Shimizu, Motohisa; Stanley, Sarah A.; Wellington, Samantha; Kazyanskaya, Edward; Hung, Deborah T. Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 22 p. 6052 - 6059

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Citation Number: 24

Abstract

Abstract In an effort to develop new and potent agents for therapy against tuberculosis, a high-throughput screen was performed against Mycobacterium tuberculosis strain H37Rv. Two 6-aryl-5, 7-dimethyl-4-phenylcoumarin compounds 1a and 1b were found with modest activity. A series of coumarin derivatives were synthesized to improve potency and to investigate the structure–activity relationship of the series. Among them, compounds 1o ...