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Renin inhibitors containing .psi.[CH2O] pseudopeptide inserts
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1988
Year
Renin InhibitorsPeptide SciencePharmacotherapyPharmaceutical ChemistryMolecular PharmacologyMedicinal ChemistryComparable PotencyBiochemistryMechanism Of ActionNeuropharmacologyNon-peptide LigandPharmacologyN-terminal Boc-protected InhibitorsNatural SciencesPeptide LibraryRational Drug DesignPeptide TherapeuticMedicineDrug Discovery
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.