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- W2016569403 abstract "The discovery of a new class of novel renin inhibitors consisting of protected dipeptide amides derived from aminoglycols (Formula I) prompted a study of structure-activity in vitro and efficacy in vivo. Thus, Boc-L-Phe-N-[(1S,2R)-1-benzyl-(2,3-dihydroxy)propyl]-L-leucinamide (1) and the corresponding histidinamide (2) inhibit human renin in vitro (IC50: 8.7 × 10−6 M and 2.6 × 10−6 M, respectively). Compound 1 has a slight inhibitory effect on pepsin and compound 2 does not inhibit pepsin at all (at 10−4M); these compounds are inactive against rat renin. Compound 1 is efficacious in lowering plasma renin activity in the Rhesus monkey (i.v.). Results indicate that this new class of low molecular weight inhibitors is specific for human renin and thus constitutes a new source of drug candidates." @default.
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- W2016569403 date "1985-10-01" @default.
- W2016569403 modified "2023-10-03" @default.
- W2016569403 title "Dipeptide glycols: A new class of renin inhibitors" @default.
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- W2016569403 doi "https://doi.org/10.1016/0006-291x(85)91001-0" @default.
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