The synoxazolidinone family of marine natural products contains an unusual 4-heterocyclic core known to possess antimicrobial and antibiofilm activity. This work expands the previously reported antimicrobial and antibiofilm SAR of synoxazolidinone analogues via late-stage nitrogen functionalization of synoxazolidinone precursors. These newly developed analogues, bearing a variety of amine moieties, were tested against ESKAPE pathogens, which are multi-drug resistant bacteria notorious for their widespread implications in nosocomial infections. Development and identification of novel natural product scaffolds, capable of exercising activity against bacterial biofilm pathways, especially against Gram-negative pathogens, is imperative. The work herein describes the synthesis of these nitrogen-functionalized synoxazolidinone derivatives and their antimicrobial activity and antibiofilm activity.

Synthesis and biological evaluation of 4-oxazolidinone antimicrobial agents

ACS Fall 2020 Virtual Meeting

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