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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Publicat a:ACS Med Chem Lett
Autors principals: 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
Format: Artigo
Idioma:Inglês
Publicat: American Chemical Society 2017
Accés en línia: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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