181716-90-5Relevant articles and documents
Bioactive hydroxyethylene dipeptide isosteres with hydrophobic (P3- P1)-moieties. A novel strategy towards small non-peptide renin inhibitors
Rasetti, Vittorio,Cohen, N. Claude,Rueeger, Heinrich,Goeschke, Richard,Maibaum, Juergen,Cumin, Frederic,Fuhrer, Walter,Wood, Jeanette M.
, p. 1589 - 1594 (2007/10/03)
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.