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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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: 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: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2017
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC5642017/
https://ncbi.nlm.nih.gov/pubmed/29057044
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.7b00196
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