title: Design, synthesis, and biological evaluation of a novel series of quercetin diacylglucosides as potent anti-MRSA and anti-VRE agents.
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.
authors.affiliation: Department of Molecular Design for Medicine, Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University, Kita-Ku, Okayama, Japan. chem.lokman@gmail.com
authors.forename: Abugafar M L
authors.initials: AM
authors.lastname: Hossion
authors.forename: Nao
authors.initials: N
authors.lastname: Otsuka
authors.forename: Rafiya K
authors.initials: RK
authors.lastname: Kandahary
authors.forename: Tomofusa
authors.initials: T
authors.lastname: Tsuchiya
authors.forename: Wakano
authors.initials: W
authors.lastname: Ogawa
authors.forename: Akimasa
authors.initials: A
authors.lastname: Iwado
authors.forename: Yoshito
authors.initials: Y
authors.lastname: Zamami
authors.forename: Kenji
authors.initials: K
authors.lastname: Sasaki
mesh_terms: D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D015195:Drug Design; D016983:Enterococcus / Q000187:drug effects*; D005960:Glucosides / Q000737:chemistry*; D055624:Methicillin-Resistant Staphylococcus aureus / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D011794:Quercetin / Q000737:chemistry / Q000494:pharmacology*; D014640:Vancomycin / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D005960:Glucosides; D014640:Vancomycin; D011794:Quercetin