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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Pubblicato in:ACS Infect Dis
Autori principali: 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
Natura: Artigo
Lingua:Inglês
Pubblicazione: American Chemical Society 2016
Accesso online: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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