Abstract

The design and synthesis of new truncated δ-amino hydroxyethylene dipeptide isosteres lacking the P 4-P 2 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, lowmolecular weight renin inhibitors with improved pharmacokinetic properties.

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