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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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Detalles Bibliográficos
Autores principales: 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.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Science Ltd 2017
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5696560/
https://www.ncbi.nlm.nih.gov/pubmed/29107541
http://dx.doi.org/10.1016/j.bmcl.2017.10.042

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