摘要
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-(a-carboxy-β-hydroxyalkyl or aralkyl)-tripeptides havebeen designed and synthesized as renin inhibitors. NBS and water were added toa-ene-acids to give erythro-α-bromo-β-hydroxy-acids, Then condensation of thelatter with Phe-Val-Tyr(Phe)OC_2H_3.HCl afforded new compounds 1~8. Details ofstereochemical determinations were also presented. The in vitro inhibition on human renin of compounds 1~8 had K_i values of0.49~1.70 mmol/L.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
1989年第12期535-538,共4页
Chinese Journal of Pharmaceuticals
基金
国家自然科学基金
关键词
肾素抑制剂
三肽酯
合成
renin inhibitor, N-(α-carboxy-β-hydroxyalkyl) tripeptide
