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设计合成了8个N-(α-羟基-β-羟基烃基)三肽酯作为肾素抑制剂。α-烯酸与NBS和水反应生成赤式的α-溴-β-羟基酸(Ⅱ),Ⅱ与Phe-Val-Tyr(Phe)OC_2H_5·HCl缩合得到的化合物1～8,都具有抑制肾素活性的作用(K_i=0.49～1.70mmol/L),并推证了它们的构型。
Eight N- (α-hydroxy-β-hydroxyalkyl) tripeptide esters were designed and synthesized as renin inhibitors. The compounds 1 to 8 obtained by the condensation of α-enoic acid with NBS and water to form the erythro-bromo-β-hydroxy acid (II) and II with Phe-Val-Tyr (Phe) OC 2 H 5 · HCl all have the inhibitory effects on the kidney (K_i = 0.49-1.70 mmol / L), and their configuration was also deduced.