Bioactive hydroxyethylene dipeptide isosteres with hydrophobic (P3- P1)-moieties. A novel strategy towards small non-peptide renin inhibitors

Article abstract of DOI:10.1016/S0960-894X(96)00279-X

The design and synthesis of new truncated δ-amino hydroxyethylene dipeptide isosteres lacking the P₄-P₂ peptide backbone is described. The most active compounds 15c and 30c inhibited human renin in the submicromolar range. This promising concept may offer the possibility to discover completely non-peptide, low-molecular weight renin inhibitors with improved pharmacokinetic properties.