Design, Synthesis, and Structure–Activity Relationship Studies of Tryptanthrins As Antitubercular Agents

…, T Oh, T Kaneko, AM Upton, SG Franzblau…

Index: Hwang, Jae-Min; Oh, Taegwon; Kaneko, Takushi; Upton, Anna M.; Franzblau, Scott G.; Ma, Zhenkun; Cho, Sang-Nae; Kim, Pilho Journal of Natural Products, 2013 , vol. 76, # 3 p. 354 - 367

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Citation Number: 25

Abstract

The natural product tryptanthrin (1a) represents a potential lead for new tuberculosis (TB) drugs since tryptanthrin and its synthetic analogues possess potent in vitro activity against Mycobacterium tuberculosis (Mtb). However, in spite of their in vitro activity, none of these agents have been shown to be efficacious in vivo against animal models of TB. Described herein are syntheses of new tryptanthrin analogues together with a systematic ...