title: Renin inhibitors containing psi[CH2O] pseudopeptide inserts.
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 X 10(-9) M.
authors.affiliation: Cardiovascular Diseases Research, Upjohn Company, Kalamazoo, Michigan 49001.
authors.forename: R E
authors.initials: RE
authors.lastname: TenBrink
authors.forename: D T
authors.initials: DT
authors.lastname: Pals
authors.forename: D W
authors.initials: DW
authors.lastname: Harris
authors.forename: G A
authors.initials: GA
authors.lastname: Johnson
mesh_terms: D000595:Amino Acid Sequence; D000808:Angiotensinogen / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D006801:Humans; D008969:Molecular Sequence Data; D013329:Structure-Activity Relationship; D000092502:Renin Inhibitors
chemical_list: D000808:Angiotensinogen; D000092502:Renin Inhibitors