具有抗糖尿病活性（拟）二肽分子的设计、合成及生物活性

采用液相缩合法，保护的苯丙氨酸衍生物和氨基葡萄糖衍生物分别与Fmoc氨基酸偶联，简便地得到9个未见报道的L-对硝基苯丙氨酸二肽衍生物4a～i和4个2-氨基-β-D-葡萄糖拟二肽衍生物8a～d，收率为52．4％～88．1％．4a～i选择性碱性水解，得到9个对应的水解产物5a～i，收率为64．4％-90．4％．产物的化学结构经1HNMR，13CNMR和HRMS表征及证实．体外抗糖尿病活性测试结果表明，某些化合物具有很强的抗糖尿病活性，其中化合物4c和8b的过氧化物酶体增殖物激活受体反应元件（PPRE）相对激动活性分别达到150．59％和185．23％，EC50分别为1．37uM和0．64uM，作为新型抗糖尿病先导分子值得进一步研究．

Design, synthesis and evaluation of （pseudo）dipeptide compounds with potential antidiabetic activity

Nine new dipeptide derivatives of L-4-nitrophenylalanine（4a-i） and four chiral N-glycosylated amino acids （Sa-d） were prepared by coupling reaction. The overall yields were 52.41%-88.08%. Nine corresponding hydrolysis products 5a-i were obtained by alkaline hydrolysis of compounds 4a-i in yields of 64.4%-90.4%. The chemical structures of these products were confirmed by 1H NMR, 13C NMR and HR MS. The peroxisome proliferator-activated receptor response element （PPRE） relative agonist activities of 4c and 8b reached 150.59% and 185.23%, the EC50 values were 1.37 uM and 0.64 uM, respectively, which exhibited excellent antidiabetic activity and thus deserved further study as lead compounds of antidiabetic agents.