In this section, you can access to the latest technical information related to the FUTURE project topic.

Design, synthesis, and biological evaluation of novel 4H-chromen-4-one derivatives as antituberculosis agents against multidrug-resistant tuberculosis

A series of 4H-chromen-4-one derivatives obtained by scaffold morphing of the benzofuran compound, TAM16, were tested for antitubercular activity. Compound 8d was active against drug-sensitive and multidrug-resistant tuberculosis. A preliminary druggability evaluation showed that compound 8d displayed favorable mouse and human microsomal stability, low cytotoxicity, and acceptable oral bioavailability. An in?vivo study indicated that compound 8d exhibited modest efficacy in an acute mouse model of TB after 3 weeks of treatment. Thus, 8d is a promising antituberculosis lead compound.

Graphical abstract

» Author: Wenting Zhao, Bin Wang, Yuke Liu, Lei Fu, Li Sheng, Hongyi Zhao, Yu Lu, Dongfeng Zhang

» Publication Date: 01/03/2020

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