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.

journal_name

J Med Chem

authors

TenBrink RE,Pals DT,Harris DW,Johnson GA

doi

10.1021/jm00398a029

subject

Has Abstract

pub_date

1988-03-01 00:00:00

pages

671-7

issue

3

eissn

0022-2623

issn

1520-4804

journal_volume

31

pub_type

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