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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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Détails bibliographiques
Publié dans:Bioorg Med Chem
Auteurs principaux: 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.
Format: Artigo
Langue:Inglês
Publié: Elsevier Science 2018
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Accès en ligne: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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