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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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Detalhes bibliográficos
Publicado no:Bioorg Med Chem
Main Authors: 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
Idioma:Inglês
Publicado em: Elsevier Science 2018
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Acesso em linha: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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