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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Publié dans:ACS Infect Dis
Auteurs principaux: 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
Langue:Inglês
Publié: American Chemical Society 2016
Accès en ligne: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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