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

✍ Scribed by Vittorio Rasetti; N.Claude Cohen; Heinrich Rüeger; Richard Göschke; Jürgen Maibaum; Frederic Cumin; Walter Fuhrer; Jeanette M. Wood

• Book ID: 104364620
• Publisher: Elsevier Science
• Year: 1996
• Tongue: English
• Weight: 426 KB
• Volume: 6
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/s0960-894x(96)00279-x

✦ Synopsis

The design and synthesis of new truncated 8-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, lowmolecular weight renin inhibitors with improved pharmacokinetic properties.