具有光学活性的葡萄糖酸尤利沙星制备及体外抗菌活性初步研究

目的将消旋的尤利沙星进行手性拆分制备葡萄糖酸左旋尤利沙星和葡萄糖酸右旋尤利沙星,并对其抗菌活性进行初步比较研究。方法采用D-和L-酒石酸手性试剂,对消旋的尤利沙星进行手性拆分得到S和R构型的尤利沙星对映体,分别与葡萄糖酸反应,制备了葡萄糖酸左旋尤利沙星和葡萄糖酸右旋尤利沙星,选择4种菌株测定其体外抗菌活性。结果葡萄糖酸左旋尤利沙星的体外抗菌活性均明显强于葡萄糖酸右旋尤利沙星或消旋的尤利沙星。结论采用手性试剂对消旋的尤利沙星进行拆分的方法可行,葡萄糖酸左旋尤利沙星有进一步研发的价值。

Preparation of optically active isomers ulifloxacin glyconate and prelimilary study on antibiotic activity in vitro

Objective To prepare the optically acive isomers of S-and R-ulifloxacin glyconate,and study the prelimilary antibiotic activity of S and R-ulifloxacin glyconate in vitro.Methods The S-or R-ulifloxacin was prepared by chiral resolution of racemic ulifloxacin with D-or L-tartaric acid,and then gone through the reactions between S and R-ulifloxacin with the glucanic acid.The antibacterial effect of S-or R-ulifloxacin was determinded by four suitable bacterial strains in vitro. Results S-and R-ulifloxacin glyconate were successfully prepared respectively.The antibiotic activity of S-ulifloxacin was significantly higher than that of R-ulifloxacin in vitro.Conclusions It is practical to use the method of chiral resolution of racemic ulifloxacin with chiral reagent.The S-ulifloxacin has further-researching potency.