PMID: 3279210Mar 1, 1988

Renin inhibitors containing psi[CH2O] pseudopeptide inserts

Journal of Medicinal Chemistry
R E TenBrinkG A Johnson

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.

Citations

Apr 1, 1990·Medicinal Research Reviews·W J Greenlee
Jan 18, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Spyridon MourtasKleomenis Barlos
Apr 1, 1990·International Journal of Peptide and Protein Research·P BretonR Mayer

Related Concepts

Renin Substrate Tetradecapeptide
Preprorenin
Structure-Activity Relationship
Physicochemical Phenomena

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