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运用“违法传递”概念,根据白念珠菌对寡肽的传送特点,设计并合成了8个含L4氧代赖氨酸(以下称I677)和N3(4甲氧基富马酰)L2,3二氨基丙酸(以下称FMDP)的寡肽类似物,均系新化合物。体外抗白念珠菌试验表明:I677FMDP肽(I677FMDP,I677AAFMDP,其中AA=Nva,Val,Leu,Phe,Pro,D,LpClPhe,DPgly)是I677单体摩尔活性的40~770倍,是FMDP的60~1130倍,其摩尔最低抑菌浓度为656×10-9~35×10-10mol·disk-1。羧肽酶A存在时化合物I677FMDP体外抗菌试验表明,含FMDP的化合物I677FMDP能抵抗羧肽酶A的酶解。
According to the transmission characteristics of Candida albicans on oligopeptides, eight L-4-oxo-lysine (hereinafter referred to as I-677) and N3 (4-methoxy Fumaric) L 2,3 diaminopropionic acid (hereinafter referred to as FMDP) oligopeptide analogues, all of the new compounds. In vitro Candida albicans test showed: I 677 FDDP peptide (I 677 FMDP, I 677 AA FMDP, including AA = Nva, Val, Leu, Phe, Pro, D, L p Cl Phe, D Pgly) I 677 monomer molar activity 40 ~ 770 times, is 60 ~ 1130 times FMDP, the molar minimum inhibitory concentration of 6 56 × 10-9 ~ 3 5 × 10- 10mol · disk-1. Carboxypeptidase A presence of compound I 677 FDM in vitro antibacterial test showed that compounds containing FMDP I 677 FMDP can resist carboxypeptidase A hydrolysis.