Ontology highlight
ABSTRACT:
SUBMITTER: Choi PJ
PROVIDER: S-EPMC5696560 | biostudies-literature | 2017 Dec
REPOSITORIES: biostudies-literature
Bioorganic & medicinal chemistry letters 20171020 23
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-pyridyl derivatives appeared to have an additional contribution to antibacterial potency. The majority of the compounds were (desirably) more polar and had higher rates of clearance than bedaquiline, and sh ...[more]