Ontology highlight
ABSTRACT:
SUBMITTER: Kurasaki H
PROVIDER: S-EPMC4904260 | biostudies-literature | 2016 Jun
REPOSITORIES: biostudies-literature
ACS medicinal chemistry letters 20160405 6
Herein we report a scaffold-hopping approach to identify a new scaffold with a zinc binding headgroup. Structural information was used to give novel oxazolidinone-based LpxC inhibitors. In particular, the most potent compound, 23j, showed a low efflux ratio, nanomolar potencies against E. coli LpxC enzyme, and excellent antibacterial activity against E. coli and K. pneumoniae. Computational docking was used to predict the interaction between 23j and E. coli LpxC, suggesting that the interactions ...[more]