… –Activity Relationships of Antitubercular Nitroimidazoles. 3. Exploration of the Linker and Lipophilic Tail of ((S)-2-Nitro-6, 7-dihydro-5 H-imidazo [2, 1-b][1, 3] oxazin-6- …

…, SB Lakshminarayana, P Niyomrattanakit…

Index: Cherian, Joseph; Choi, Inhee; Nayyar, Amit; Manjunatha, Ujjini H.; Mukherjee, Tathagata; Lee, Yong Sok; Boshoff, Helena I.; Singh, Ramandeep; Ha, Young Hwan; Goodwin, Michael; Lakshminarayana, Suresh B.; Niyomrattanakit, Pornwaratt; Jiricek, Jan; Ravindran, Sindhu; Dick, Thomas; Keller, Thomas H.; Dartois, Veronique; Barry III, Clifton E. Journal of Medicinal Chemistry, 2011 , vol. 54, # 16 p. 5639 - 5659

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Citation Number: 20

Abstract

The (S)-2-nitro-6-(4-(trifluoromethoxy) benzyloxy)-6, 7-dihydro-5 H-imidazo [2, 1-b][1, 3] oxazine named PA-824 (1) has demonstrated antitubercular activity in vitro and in animal models and is currently in clinical trials. We synthesized derivatives at three positions of the 4-(trifluoromethoxy) benzylamino tail, and these were tested for whole-cell activity against both replicating and nonreplicating Mycobacterium tuberculosis (Mtb). In addition, we ...