基于联烯片段的黄酮衍生物的设计、合成及抗菌活性研究

Design,synthesis of flavonoid ethers with allene fragments and their antimicrobial activities study

通过有机合成的手段合成了12个新的未保护的黄酮衍生物。该类衍生物是由天然黄酮与酯基联烯进行选择性分子加成,使联烯和黄酮羟基之间形成了C(sp2)—O键得到的。利用1 H NMR,13 C NMR,NOE和MS确定了目标化合物结构。通过96孔板法测定金黄色葡萄球菌(25923)、枯草芽孢杆菌、大肠杆菌、MrSA的MIC值,其MIC值均大于128μg/mL。上述研究结果将为制备具有药用潜力的黄酮衍生物提供理论基础。

Twelve new ethers derivatives flavonoids were designed and synthesized without the use of protective groups.Here,we report some methods developed for increasing the drug-ability of flavonoids by forging C(sp 2)—Obonds of hydroxyl groups of flavonoids with ethyl-2,3-butadienoate allenes tOobtain some new derivatives.Their structures were characterized by 1 H-,13 C-NMR,NOE,and MS spectra.Furthermore,the antimicrobial capabilities of the target compounds were measured by the 96-well plate method.All target compounds were evaluated for antimicrobial activities of Staphyloccocus aureus,Bacillus subtilis,Escherichia coli and MrSA in vitro,but their minimal inhibitory concentration(MIC)values were more than 128μg/mL.Those study will facilitate the preparation or late-stage modification of complex flavonoids for drug discovery.