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  • Title: Pepstatin analogues as novel renin inhibitors.
    Author: Guégan R, Diaz J, Cazaubon C, Beaumont M, Carlet C, Clément J, Demarne H, Mellet M, Richaud JP, Segondy D.
    Journal: J Med Chem; 1986 Jul; 29(7):1152-9. PubMed ID: 3543358.
    Abstract:
    Pepstatin analogues corresponding to the general formula A-X-Y-Sta-Ala-Sta-R were synthesized in solution phase. Various changes in the nature of the A, X, and Y groups were made to improve the inhibitory potency against human plasma renin activity. The results were interpreted by use of the active-site model based on the sequence of human angiotensinogen. The tert-butyloxycarbonyl group and the isovaleryl group were found to be the most effective acyl groups (A). The analogues having a Phe residue in place of Val1 (X) and His or amino acid with an aliphatic side chain such as norleucine or norvaline in the Y position showed the highest inhibition of human plasma renin activity with IC50 values of about 10(-8)M. Esterification or amidification of the carboxyl group of the C-terminal statine did not change the inhibitory potency. The selectivity for rat, dog, pig, and monkey plasma renin of the most interesting compounds was studied.
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