Discovery, synthesis, and biological evaluation of piperidinol analogs with anti-tuberculosis activity.
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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-(trifluoromethyl) phenoxy)-2-hydroxypropyl)-4-(4-chloro-3-(trifluoromethyl) phenyl) piperidin-4-ol demonstrated good anti-tuberculosis activity. Unfortunately, side effects were observed upon in vivo anti-tuberculosis testing of these compounds precluding their further advancement, which may be in part due to the secondary pharmacology associated with the aryl piperidinol core.
Sun, D., Scherman, M. S., Jones, V., Hurdle, J. G., Woolhiser, L. K., Knudson, S. E., ... Lee, R. E.
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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