Marinopyrrole derivatives as potential antibiotic agents against methicillin-resistant Staphylococcus aureus (III)

Yan Liu, Nina M. Haste, Wdee Thienphrapa, Jerry Li, Victor Nizet, Mary Hensler, Rongshi Li

Research output: Contribution to journalArticle

11 Scopus citations

Abstract

The marine natural product, marinopyrrole A (1), was previously shown to have significant antibiotic activity against Gram-positive pathogens, including methicillin-resistant Staphylococcus aureus (MRSA). Although compound (1) exhibits a significant reduction in MRSA activity in the presence of human serum, we have identified key modifications that partially restore activity. We previously reported our discovery of a chloro-derivative of marinopyrrole A (1a) featuring a 2-4 fold improved minimum inhibitory concentration (MIC) against MRSA, significantly less susceptibility to serum inhibition and rapid and concentration-dependent killing of MRSA. Here, we report a novel fluoro-derivative of marinopyrrole A (1e) showing an improved profile of potency, less susceptibility to serum inhibition, as well as rapid and concentration-dependent killing of MRSA.

Original languageEnglish (US)
Pages (from-to)2458-2470
Number of pages13
JournalMarine Drugs
Volume12
Issue number5
DOIs
StatePublished - May 2014

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Keywords

  • Antibiotics
  • MRSA
  • Non-symmetrical marinopyrroles
  • SAR

ASJC Scopus subject areas

  • Drug Discovery

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