Structure-Uptake Relationship Studies of Oxazolidinones in Gram-Negative ESKAPE Pathogens.

ABSTRACT: The clinical success of linezolid for treating Gram-positive infections paired with the high conservation of bacterial ribosomes predicts that if oxazolidinones were engineered to accumulate in Gram-negative bacteria, then this pharmacological class would find broad utility in eradicating infections. Here, we report an investigative study of a strategically designed library of oxazolidinones to determine the effects of molecular structure on accumulation and biological activity. Escherichia coli, Acinetobacter baumannii, and Pseudomonas aeruginosa strains with varying degrees of compromise (in efflux and outer membrane) were used to identify motifs that hinder permeation across the outer membrane and/or enhance efflux susceptibility broadly and specifically between spe

SUBMITTER: Hu Z 

PROVIDER: S-EPMC9942527 | biostudies-literature | 2022 Oct

REPOSITORIES: biostudies-literature