血管紧张素转化酶抑制剂——膦三肽的合成

Synthesis of Phosphonotripeptides as the Inhibitors of ACE

由Ｎ－保护α－氨基烃基膦酰氯与氨端游离的二肽缩合，合成了一系列具有血管紧张素转化酶（ＡＣＥ）抑制活性的膦三肽化合物．差向异构的膦三肽可用反相柱Ｎｕｃｌｅｏｓｉｌ－Ｃ１８层析分离，并利用３１Ｐ－ＮＭＲ推定未定手性中心的构型．测定了系列抑制剂的体外半抑制活性常数ＩＣ５０．

A series of phosphonotripeptides tried as the inhibitors of ACE was prepared by the condensation of the corresponding N protected α aminoalkylphosphonic chloride with N deprotected dipeptides.The epimeric phosphonotripeptides could be separated by RP HPLC and the configurations of the unknown chiral centers were assumed by 31 P NMR.The in vitro inhibition activities of the serial inhibitors toward ACE were also determined.