Synthesis and evaluation of analogues of the tuberculosis drug bedaquiline containing heterocyclic B-ring units

Analogues of bedaquiline where the phenyl B-unit was replaced with monocyclic heterocycles of widely differing lipophilicity (thiophenes, furans, pyridines) were synthesised and evaluated. While there was an expected broad positive correlation between lipophilicity and anti-TB activity, the 4-pyridy...

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Foilsithe in:Bioorg Med Chem Lett
Main Authors: Choi, Peter J., Sutherland, Hamish S., Tong, Amy S.T., Blaser, Adrian, Franzblau, Scott G., Cooper, Christopher B., Lotlikar, Manisha U., Upton, Anna M., Guillemont, Jerome, Motte, Magali, Queguiner, Laurence, Andries, Koen, Van den Broeck, Walter, Denny, William A., Palmer, Brian D.
Formáid: Artigo
Teanga:Inglês
Foilsithe: Elsevier Science Ltd 2017
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Article
Rochtain Ar Líne:https://ncbi.nlm.nih.gov/pmc/articles/PMC5696560/
https://ncbi.nlm.nih.gov/pubmed/29107541
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1016/j.bmcl.2017.10.042
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