论文部分内容阅读
目的设计合成一系列新型L-异谷氨酰胺类衍生物,并测定其对氨肽酶N(APN)的抑制活性。方法以L-谷氨酸为基本骨架,经与3,4-二氯苯甲酸反应得到关键中间体环状酸酐,再经氨解反应合成目标化合物。采用体外抑酶试验测定化合物抑制氨肽酶N的活性。结果与结论合成了15个未见报道的L-异谷氨酰胺衍生物,其结构经1H-NMR、MS、和IR谱确证。其中化合物Ⅱ4、Ⅱ6显示出较好的抑制氨肽酶N的活性(IC50=20～40μmol.L-1),有进一步研究的价值。
Aim To design and synthesize a series of new L-isoglutamine derivatives and determine the inhibitory activity against aminopeptidase N (APN). Methods L-glutamic acid was used as the basic framework to obtain the key intermediate cyclic anhydride by reaction with 3,4-dichlorobenzoic acid. The target compound was synthesized by aminolysis. Compounds were tested for their ability to inhibit aminopeptidase N activity using in vitro protease inhibition assays. RESULTS AND CONCLUSIONS Fifteen non-reported L-isoglutamine derivatives were synthesized and their structures were confirmed by 1H-NMR, MS and IR spectra. Among them, compounds Ⅱ4 and Ⅱ6 showed better activity of inhibiting aminopeptidase N (IC50 = 20 ~ 40μmol.L-1), which could be further studied.