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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...
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. |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
Elsevier Science Ltd
2017
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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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