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...

Celý popis

Uloženo v:
Podrobná bibliografie
Vydáno v:Bioorg Med Chem Lett
Hlavní autoři: 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.
Médium: Artigo
Jazyk:Inglês
Vydáno: Elsevier Science Ltd 2017
Témata:
Article
On-line přístup: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
Tagy: Přidat tag
Žádné tagy, Buďte první, kdo otaguje tento záznam!

Podobné jednotky