Natural product derivatives with bactericidal activity against Gram-positive pathogens including methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecalis.
PMID 20801034 · Bioorganic & medicinal chemistry letters · 2010 · DOI 10.1016/j.bmcl.2010.06.146
Authors: Joshua B Phillips; Adrienne E Smith; Brian R Kusche; Bradley A Bessette; P Whitney Swain; Stephen C Bergmeier; Mark C McMills; Dennis L Wright; Nigel D Priestley
Abstract
We have shown that the intentional engineering of a natural product biosynthesis pathway is a useful way to generate stereochemically complex scaffolds for use in the generation of combinatorial libraries that capture the structural features of both natural products and synthetic compounds. Analysis of a prototype library based upon nonactic acid lead to the discovery of triazole-containing nonactic acid analogs, a new structural class of antibiotic that exhibits bactericidal activity against drug resistant, Gram-positive pathogens including Staphylococcus aureus and Enterococcus faecalis.
Anti-Bacterial Agents; Biological Products; Drug Resistance, Bacterial; Enterococcus faecalis; Gram-Positive Bacteria; Macrolides; Methicillin-Resistant Staphylococcus aureus; Microbial Sensitivity Tests; Stereoisomerism; Triazoles; Vancomycin
Cite
Joshua B Phillips; Adrienne E Smith; Brian R Kusche; Bradley A Bessette; P Whitney Swain; Stephen C Bergmeier; Mark C McMills; Dennis L Wright; Nigel D Priestley. Natural product derivatives with bactericidal activity against Gram-positive pathogens including methicillin-resistant Staphylococcus aureus and vancomycin-resistant Enterococcus faecalis. Bioorganic & medicinal chemistry letters (2010). PMID 20801034. DOI 10.1016/j.bmcl.2010.06.146.