Discovery, synthesis, and biological evaluation of piperidinol analogs with anti-tuberculosis activity

…, V Jones, JG Hurdle, LK Woolhiser, SE Knudson…

Index: Sun, Dianqing; Scherman, Michael S.; Jones, Victoria; Hurdle, Julian G.; Woolhiser, Lisa K.; Knudson, Susan E.; Lenaerts, Anne J.; Slayden, Richard A.; McNeil, Michael R.; Lee, Richard E. Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 10 p. 3588 - 3594

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Citation Number: 16

Abstract

Direct anti-tuberculosis screening of commercially available compound libraries identified a novel piperidinol with interesting anti-tuberculosis activity and drug like characteristics. To generate a structure activity relationship about this hit a 22 member optimization library was generated using parallel synthesis. Products of this library 1-((R)-3-(4-chlorophenoxy)-2- hydroxypropyl)-4-(4-chloro-3-(trifluoromethyl) phenyl) piperidin-4-ol and 1-((S)-3-(4-( ...