title: Enhanced potency dipeptide glycol renin inhibitors: studies in vitro and in the conscious rhesus.
abstract: We prepared a series of novel dipeptide amides of the formula Boc-Phe-Leu-X, where X is a 3-amino-3-alkyl-1,2-propanediol with lower alkyl substitutions at C-1, in order to probe accessory binding sites in the enzyme renin. This approach was successful in generating potent inhibitors of human and hog renin in vitro. Moreover, these inhibitors were able to effect in vivo reduction of plasma renin activity (PRA) in the conscious salt-depleted rhesus monkey (i.v. route); this effect was related to the size of the C-1 alkyl group.
authors.forename: G J
authors.initials: GJ
authors.lastname: Hanson
authors.forename: J S
authors.initials: JS
authors.lastname: Baran
authors.forename: H S
authors.initials: HS
authors.lastname: Lowrie
authors.forename: S J
authors.initials: SJ
authors.lastname: Sarussi
authors.forename: P C
authors.initials: PC
authors.lastname: Yang
authors.forename: M
authors.initials: M
authors.lastname: Babler
authors.forename: S E
authors.initials: SE
authors.lastname: Bittner
authors.forename: S E
authors.initials: SE
authors.lastname: Papaioannou
authors.forename: G M
authors.initials: GM
authors.lastname: Walsh
mesh_terms: D000818:Animals; D004151:Dipeptides / Q000494:pharmacology*; D006801:Humans; D007700:Kinetics; D013045:Species Specificity; D013329:Structure-Activity Relationship; D013552:Swine; D000092502:Renin Inhibitors
chemical_list: D004151:Dipeptides; D000092502:Renin Inhibitors