From serendipity to rational antituberculosis drug discovery of mefloquine-isoxazole carboxylic acid esters

J Mao, H Yuan, Y Wang, B Wan, M Pieroni…

Index: Mao, Jialin; Yuan, Hai; Wang, Yuehong; Wan, Baojie; Pieroni, Marco; Huang, Qingqing; Van Breemen, Richard B.; Kozikowski, Alan P.; Franzblau, Scott G. Journal of Medicinal Chemistry, 2009 , vol. 52, # 22 p. 6966 - 6978

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Citation Number: 39

Abstract

Both in vitro and in vivo metabolism studies suggested that 5-(2, 8-bis (trifluoromethyl) quinolin-4-yloxymethyl) isoxazole-3-carboxylic acid ethyl ester (compound 3) with previously reported antituberculosis activity is rapidly converted to two metabolites 3a and 3b. In order to improve the metabolic stability of this series, chemistry efforts were focused on the modification of the oxymethylene linker of compound 3 in the present study. Compound 9d ...

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