2(5H)-吡咯酮衍生物的合成及对铜绿假单胞菌生物膜的体外作用

Synthesis of 2(5H)-pyrrinones and the inhibitory effects on the Biofilms of P.aeruginosa in vitro

以乙酰乙酸乙酯为原料,设计合成2(5H)-吡咯酮及其衍生物,所得化合物经1H NMR、13C NMR、MS和元素分析等确证.通过扫描电镜观察2(5H)-吡咯酮对黏液型铜绿假单胞菌P.aeruginosa(PA)体外生物被膜(bio-films,BF)的影响,可见BF被破坏,基质样物变稀疏,细菌群聚大为降低.活性实验结果表明,2(5H)-吡咯酮类化合物具有一定的抑制细菌群体感应的能力.

A series of pyrroles and 2 （SH）-pyrrinones were successfully synthesized from ethyl acetoacetate, and characterized by ^1H NMR, ^13C NMR, MS spectra and elemental analysis. Scanning electron microscope （SEM） was used to evaluate the effects of the 2 （5H）-pyrrolones on the quorum sensing （QS） system and the bacterial biofilm （BF） formation biofilm formation. The biofilms of P. aeruginosa were inhibited, the base became sparseness, and the swarming was decreased. The results of biological activity tests indicated that 2 （5H）-pyrrinones showed potent ability to inhibit the formation of bacterial biofilms.