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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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Detalles Bibliográficos
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: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Science 2018
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5933462/
https://www.ncbi.nlm.nih.gov/pubmed/29482950
http://dx.doi.org/10.1016/j.bmc.2018.02.026