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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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Detalles Bibliográficos
Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2016
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5108244/
https://www.ncbi.nlm.nih.gov/pubmed/27627628
http://dx.doi.org/10.1021/acsinfecdis.6b00036