Renin inhibitors containing .psi.[CH2O] pseudopeptide inserts
- 1 March 1988
- journal article
- research article
- Published by American Chemical Society (ACS) in Journal of Medicinal Chemistry
- Vol. 31 (3) , 671-677
- https://doi.org/10.1021/jm00398a029
Abstract
Renin inhibitors 2-4 with the D-Lys renin inhibitory peptide (RIP) sequence, but containing Leu.psi.[CH2O]Ala (2), Leu.psi.[CH2O]Val (3), and Leu.psi.[CH2O]Leu (4) at the P1-P1'' site, were of a comparable potency to RIP. N-Terminal Boc-protected inhibitors containing Pro.psi.[CH2O]Phe in positions P4-P3 were potent inhibitors of renin, with Boc-Phe-Pro.psi.[CH2O]Phe-His-Leu.psi.[CH(OH)CH2]Val-Ile-(2-aminomethyl)pyridine (17) having an IC50 of 1.6 .times. 10-9 M.This publication has 2 references indexed in Scilit:
- A method for the preparation of stereochemically defined .psi.[CH2O] pseudodipeptidesThe Journal of Organic Chemistry, 1987
- Design and synthesis of a potent and specific renin inhibitor with a prolonged duration of action in vivoJournal of Medicinal Chemistry, 1986