Design, synthesis, and biological evaluation of a novel series of quercetin diacylglucosides as potent anti-MRSA and anti-VRE agents.
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.
Hossion
Abugafar M L
AM
Department of Molecular Design for Medicine, Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University, Kita-Ku, Okayama, Japan. chem.lokman@gmail.com
Otsuka
Nao
N
Kandahary
Rafiya K
RK
Tsuchiya
Tomofusa
T
Ogawa
Wakano
W
Iwado
Akimasa
A
Zamami
Yoshito
Y
Sasaki
Kenji
K
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*
D000900:Anti-Bacterial Agents; D005960:Glucosides; D014640:Vancomycin; D011794:Quercetin