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

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Research output: Contribution to journal › Article

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 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

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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Hossion, A. M. L., Otsuka, N., Kandahary, R. K., Tsuchiya, T., Ogawa, W., Iwado, A., Zamami, Y., & Sasaki, K. (2010). Design, synthesis, and biological evaluation of a novel series of quercetin diacylglucosides as potent anti-MRSA and anti-VRE agents. Bioorganic and Medicinal Chemistry Letters, 20(17), 5349-5352. https://doi.org/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. / Hossion, Abugafar M.L.; Otsuka, Nao; Kandahary, Rafiya K.; Tsuchiya, Tomofusa; Ogawa, Wakano; Iwado, Akimasa; Zamami, Yoshito; Sasaki, Kenji.

In: Bioorganic and Medicinal Chemistry Letters, Vol. 20, No. 17, 01.09.2010, p. 5349-5352.

Research output: Contribution to journal › Article

Hossion, Abugafar M.L. ; Otsuka, Nao ; Kandahary, Rafiya K. ; Tsuchiya, Tomofusa ; Ogawa, Wakano ; Iwado, Akimasa ; Zamami, Yoshito ; Sasaki, Kenji. / Design, synthesis, and biological evaluation of a novel series of quercetin diacylglucosides as potent anti-MRSA and anti-VRE agents. In: Bioorganic and Medicinal Chemistry Letters. 2010 ; Vol. 20, No. 17. pp. 5349-5352.

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