Simple synthesis of endophenazine G and other phenazines and their evaluation as anti-methicillin-resistant Staphylococcus aureus agents

Martin Conda Sheridan, Venkatareddy Udumula, Jennifer L. Endres, Caleb N. Harper, Lee Jaramillo, Haizhen Andrew Zhong, Kenneth W Bayles

Research output: Contribution to journalArticle

12 Citations (Scopus)

Abstract

Community-associated methicillin resistant Staphylococcus aureus (CA-MRSA) has become a severe health concern because of its treatment difficulties. Herein, we report the synthesis and biological evaluation of two phenazine natural products and a series of phenazines that show promising activities against MRSA with MIC values in the low micromolar range. Basic studies revealed that these compounds are bacteriostatic agents. The most active compound also displayed promising IC50 values against HaCat cells. Finally, a QSAR model was developed to understand the key structural features of the molecules.

Original languageEnglish (US)
Pages (from-to)710-721
Number of pages12
JournalEuropean Journal of Medicinal Chemistry
Volume125
DOIs
StatePublished - Jan 1 2017

Fingerprint

Phenazines
Methicillin
Methicillin-Resistant Staphylococcus aureus
Biological Products
Health
Molecules
Quantitative Structure-Activity Relationship
Inhibitory Concentration 50
phenazine

Keywords

  • Antibacterial Agents
  • Bacterial Infections
  • Drug-resistant Bacteria
  • MRSA
  • Methicillin-Resistant Staphylococcus Aureus
  • Natural Product Synthesis
  • Phenazines

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

Cite this

Simple synthesis of endophenazine G and other phenazines and their evaluation as anti-methicillin-resistant Staphylococcus aureus agents. / Conda Sheridan, Martin; Udumula, Venkatareddy; Endres, Jennifer L.; Harper, Caleb N.; Jaramillo, Lee; Zhong, Haizhen Andrew; Bayles, Kenneth W.

In: European Journal of Medicinal Chemistry, Vol. 125, 01.01.2017, p. 710-721.

Research output: Contribution to journalArticle

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