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

doi:10.1016/j.bmcl.2010.02.060

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 journal › Article › peer-review

21 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 language	English
Pages (from-to)	5349-5352
Number of pages	4
Journal	Bioorganic and Medicinal Chemistry Letters
Volume	20
Issue number	17
DOIs	https://doi.org/10.1016/j.bmcl.2010.02.060
Publication status	Published - Sep 1 2010
Externally published	Yes

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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10.1016/j.bmcl.2010.02.060

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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.",

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AU - Hossion, Abugafar M.L.

AU - Otsuka, Nao

AU - Kandahary, Rafiya K.

AU - Tsuchiya, Tomofusa

AU - Ogawa, Wakano

AU - Iwado, Akimasa

AU - Zamami, Yoshito

AU - Sasaki, Kenji

PY - 2010/9/1

Y1 - 2010/9/1

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AB - 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.

KW - Antibacterials

KW - Multi-drug resistance

KW - Quercetin-3-glucoside

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

Abstract

Keywords

ASJC Scopus subject areas

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