Department of Molecular Design for Medicine, Graduate School of Medicine, Dentistry and Pharmaceutical Sciences, Okayama University, Kita-Ku, Okayama, Japan.
Bioorg Med Chem Lett. 2010 Sep 1;20(17):5349-52. doi: 10.1016/j.bmcl.2010.02.060. Epub 2010 Feb 19.
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.
基于对 MRSA 菌株抑制天然化合物 A 的研究，我们通过 Steglich 酯化反应设计并首次合成了一系列新型槲皮素二酰基葡萄糖苷。我们对不同的多药耐药菌和大肠杆菌 DNA 拓扑异构酶 B 的体外抑制活性进行了研究。在该系列化合物中，化合物 10h 对万古霉素耐药肠球菌的活性比化合物 A 高 128 倍，比化合物 A 更有效，这表明它是一种很有前途的新型抗 MRSA 和抗 VRE 候选药物。
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