Bioactive hydroxyethylene dipeptide isosteres with hydrophobic (P3-P1)-moieties. A novel strategy towards small non-peptide renin inhibitors
1996; Elsevier BV; Volume: 6; Issue: 13 Linguagem: Inglês
10.1016/s0960-894x(96)00279-x
ISSN1464-3405
AutoresVittorio Rasetti, N.C. Cohen, H. Rüeger, Richard Göschke, Jürgen Maibaum, Frédéric Cumin, Walter Fuhrer, Jeanette M. Wood,
Tópico(s)Phosphodiesterase function and regulation
ResumoThe 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, lowmolecular weight renin inhibitors with improved pharmacokinetic properties.
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