Renin inhibitors containing psi[CH2O] pseudopeptide inserts |
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| Authors: | R E TenBrink D T Pals D W Harris G A Johnson |
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| Institution: | Cardiovascular Diseases Research, Upjohn Company, Kalamazoo, Michigan 49001. |
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| Abstract: | Renin inhibitors 2-4 with the D-Lys renin inhibitory peptide (RIP) sequence, but containing Leu psiCH2O]Ala (2), Leu psiCH2O]Val (3), and Leu psiCH2O]Leu (4) at the P1-P1' site, were of a comparable potency to RIP. N-Terminal Boc-protected inhibitors containing Pro psiCH2O]Phe in positions P4-P3 were potent inhibitors of renin, with Boc-Phe-Pro psiCH2O]Phe-His-Leu psiCH(OH)CH2]Val-Ile-(2-aminomethyl) pyridine (17) having an IC50 of 1.6 X 10(-9) M. |
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