3,5-Dialkoxypyridine analogues of bedaquiline are potent antituberculosis agents with minimal inhibition of the hERG channel

Bedaquiline is a new drug of the diarylquinoline class that has proven to be clinically effective against drug-resistant tuberculosis, but has a cardiac liability (prolongation of the QT interval) due to its potent inhibition of the cardiac potassium channel protein hERG. Bedaquiline is highly lipop...

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Veröffentlicht in:Bioorg Med Chem
Hauptverfasser: Sutherland, Hamish S., Tong, Amy S.T., Choi, Peter J., Blaser, Adrian, Conole, Daniel, Franzblau, Scott G., Lotlikar, Manisha U., Cooper, Christopher B., Upton, Anna M., Denny, William A., Palmer, Brian D.
Format: Artigo
Sprache:Inglês
Veröffentlicht: Elsevier Science 2019
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Article
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC6467547/
https://ncbi.nlm.nih.gov/pubmed/30803745
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmc.2019.02.026
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