Structure-activity relationships for analogs of the tuberculosis drug bedaquiline with the naphthalene unit replaced by bicyclic heterocycles

Replacing the naphthalene C-unit of the anti-tuberculosis drug bedaquiline with a range of bicyclic heterocycles of widely differing lipophilicity gave analogs with a 4.5-fold range in clogP values. The biological results for these compounds indicate on average a lower clogP limit of about 5.0 in th...

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Publicado en:Bioorg Med Chem
Autores principales: Sutherland, Hamish S., Tong, Amy S.T., Choi, Peter J., Conole, Daniel, Blaser, Adrian, Franzblau, Scott G., Cooper, Christopher B., Upton, Anna M., Lotlikar, Manisha U., Denny, William A., Palmer, Brian D.
Formato: Artigo
Lenguaje:Inglês
Publicado: Elsevier Science 2018
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Article
Acceso en línea:https://ncbi.nlm.nih.gov/pmc/articles/PMC5933462/
https://ncbi.nlm.nih.gov/pubmed/29482950
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmc.2018.02.026
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