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 Citations (Scopus)

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

Fingerprint

Methicillin-Resistant Staphylococcus aureus
Anti-Bacterial Agents
Serum
Microbial Sensitivity Tests
Biological Products
marinopyrrole A

Keywords

  • Antibiotics
  • MRSA
  • Non-symmetrical marinopyrroles
  • SAR

ASJC Scopus subject areas

  • Drug Discovery

Cite this

Marinopyrrole derivatives as potential antibiotic agents against methicillin-resistant Staphylococcus aureus (III). / Liu, Yan; Haste, Nina M.; Thienphrapa, Wdee; Li, Jerry; Nizet, Victor; Hensler, Mary; Li, Rongshi.

In: Marine Drugs, Vol. 12, No. 5, 05.2014, p. 2458-2470.

Research output: Contribution to journalArticle

Liu, Yan ; Haste, Nina M. ; Thienphrapa, Wdee ; Li, Jerry ; Nizet, Victor ; Hensler, Mary ; Li, Rongshi. / Marinopyrrole derivatives as potential antibiotic agents against methicillin-resistant Staphylococcus aureus (III). In: Marine Drugs. 2014 ; Vol. 12, No. 5. pp. 2458-2470.
@article{ccd7364912524fd8836f1673059c8c39,
title = "Marinopyrrole derivatives as potential antibiotic agents against methicillin-resistant Staphylococcus aureus (III)",
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.",
keywords = "Antibiotics, MRSA, Non-symmetrical marinopyrroles, SAR",
author = "Yan Liu and Haste, {Nina M.} and Wdee Thienphrapa and Jerry Li and Victor Nizet and Mary Hensler and Rongshi Li",
year = "2014",
month = "5",
doi = "10.3390/md12052458",
language = "English (US)",
volume = "12",
pages = "2458--2470",
journal = "Marine Drugs",
issn = "1660-3397",
publisher = "Multidisciplinary Digital Publishing Institute (MDPI)",
number = "5",

}

TY - JOUR

T1 - Marinopyrrole derivatives as potential antibiotic agents against methicillin-resistant Staphylococcus aureus (III)

AU - Liu, Yan

AU - Haste, Nina M.

AU - Thienphrapa, Wdee

AU - Li, Jerry

AU - Nizet, Victor

AU - Hensler, Mary

AU - Li, Rongshi

PY - 2014/5

Y1 - 2014/5

N2 - 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.

AB - 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.

KW - Antibiotics

KW - MRSA

KW - Non-symmetrical marinopyrroles

KW - SAR

UR - http://www.scopus.com/inward/record.url?scp=84901452761&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=84901452761&partnerID=8YFLogxK

U2 - 10.3390/md12052458

DO - 10.3390/md12052458

M3 - Article

C2 - 24796304

AN - SCOPUS:84901452761

VL - 12

SP - 2458

EP - 2470

JO - Marine Drugs

JF - Marine Drugs

SN - 1660-3397

IS - 5

ER -