Design, synthesis, and biological evaluation of a novel series of quercetin diacylglucosides as potent anti-MRSA and anti-VRE agents

Abugafar M.L. Hossion, Nao Otsuka, Rafiya K. Kandahary, Tomofusa Tsuchiya, Wakano Ogawa, Akimasa Iwado, Yoshito Zamami, Kenji Sasaki

Research output: Contribution to journalArticle

19 Citations (Scopus)

Abstract

A series of novel quercetin diacylglucosides were designed and first synthesized by Steglich esterification on the basis of MRSA strains inhibiting natural compound A. The in vitro inhibition of different multi-drug resistant bacterial strains and Escherichia coli DNA gyrase B was investigated. In the series, compound 10h was up to 128-fold more potent against vancomycin-resistant enterococci and more effective than A, which represents a promising new candidate as a potent anti-MRSA and anti-VRE agent.

Original languageEnglish
Pages (from-to)5349-5352
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume20
Issue number17
DOIs
Publication statusPublished - Sep 1 2010

Keywords

  • Antibacterials
  • Multi-drug resistance
  • Quercetin-3-glucoside

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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