5-Fluoroimidazo[4,5-b]pyridine Is a Privileged Fragment That Conveys Bioavailability to Potent Trypanosomal Methionyl-tRNA Synthetase Inhibitors

[Image: see text] Fluorination is a well-known strategy for improving the bioavailability of drug molecules. However, its impact on efficacy is not easily predicted. On the basis of inhibitor-bound protein crystal structures, we found a beneficial fluorination spot for inhibitors targeting methionyl...

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Udgivet i:ACS Infect Dis
Main Authors: Zhang, Zhongsheng, Koh, Cho Yeow, Ranade, Ranae M., Shibata, Sayaka, Gillespie, J. Robert, Hulverson, Matthew A., Huang, Wenlin, Nguyen, Jasmine, Pendem, Nagendar, Gelb, Michael H., Verlinde, Christophe L. M. J., Hol, Wim G. J., Buckner, Frederick S., Fan, Erkang
Format: Artigo
Sprog:Inglês
Udgivet: American Chemical Society 2016
Online adgang:https://ncbi.nlm.nih.gov/pmc/articles/PMC5108244/
https://ncbi.nlm.nih.gov/pubmed/27627628
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsinfecdis.6b00036
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