Structure− activity relationships of antitubercular nitroimidazoles. 2. Determinants of aerobic activity and quantitative structure− activity relationships

P Kim, S Kang, HI Boshoff, J Jiricek…

Index: Kim, Pilho; Zhang, Liang; Manjunatha, Ujjini H.; Singh, Ramandeep; Patel, Sejal; Jiricek, Jan; Keller, Thomas H.; Boshoff, Helena I.; Barry III, Clifton E.; Dowd, Cynthia S. Journal of Medicinal Chemistry, 2009 , vol. 52, # 5 p. 1317 - 1328

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Citation Number: 73

Abstract

The (S)-2-nitro-6-substituted 6, 7-dihydro-5 H-imidazo [2, 1-b][1, 3] oxazines have been extensively explored for their potential use as new antituberculars based on their excellent bactericidal properties on aerobic whole cells of Mycobacterium tuberculosis. An oxygen atom at the 2-position of the imidazole ring is required for aerobic activity. Here, we show that substitution of this oxygen by either nitrogen or sulfur yielded equipotent analogues. ...