Nyéki O, Szalay K S, Kisfaludy L, Kárpáti E, Szporny L, Makara G B, Varga B
Chemical Works of Gedeon Richter, Ltd., Budapest, Hungary.
J Med Chem. 1987 Oct;30(10):1719-24. doi: 10.1021/jm00393a006.
Six angiotensin II antagonists containing cyclohexylglycine (Chg) or cyclopentylglycine (Cpg) in position 5 were synthesized by stepwise elongation in solution, using the pentafluorophenyl ester method. The influence of substitution on the inhibitory properties of the analogues was studied in four different bioassays. [Sar1,Chg5,Lac8]AII proved to be the most potent antagonist with low intrinsic activity in both the in vitro and in vivo tests.
采用五氟苯基酯法，通过溶液中的逐步延伸反应，合成了6种在5位含有环己基甘氨酸（Chg）或环戊基甘氨酸（Cpg）的血管紧张素II拮抗剂。在4种不同的生物测定中研究了取代基对类似物抑制特性的影响。[Sar1,Chg5,Lac8]AII在体外和体内试验中均被证明是具有低内在活性的最有效拮抗剂。
