Synthesis of angiotensin II antagonists with variations in position 5
- 1 October 1987
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 30 (10) , 1719-1724
- https://doi.org/10.1021/jm00393a006
Abstract
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 [rats and rabbits] tests.This publication has 2 references indexed in Scilit:
- Synthesis of angiotensin II antagonists by incorporating .alpha.-methylalanine or O-methylthreonine residues in angiotensin II analogsJournal of Medicinal Chemistry, 1977
- 1,8-Disubstituted Analogues of [Ile5] and [Val5]Angiotensin II: Difference in Potency and Specificity of Angiotensin II-Antagonistic ActivityHoppe-Seyler´s Zeitschrift Für Physiologische Chemie, 1976