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6-Cyano Analogues of Bedaquiline as Less Lipophilic and Potentially Safer Diarylquinolines for Tuberculosis

[Image: see text] Bedaquiline (1) is a new drug for tuberculosis and the first of the diarylquinoline class. It demonstrates excellent efficacy against TB but induces phospholipidosis at high doses, has a long terminal elimination half-life (due to its high lipophilicity), and exhibits potent hERG c...

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Detalles Bibliográficos
Autores principales: Tong, Amy S. T., Choi, Peter J., Blaser, Adrian, Sutherland, Hamish S., Tsang, Sophia K. Y., Guillemont, Jerome, Motte, Magali, Cooper, Christopher B., Andries, Koen, Van den Broeck, Walter, Franzblau, Scott G., Upton, Anna M., Denny, William A., Palmer, Brian D., Conole, Daniel
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2017
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5642017/
https://www.ncbi.nlm.nih.gov/pubmed/29057044
http://dx.doi.org/10.1021/acsmedchemlett.7b00196