Abstract Tri-and tetrapeptides with C-terminal 1-amino-1-cycloalkanecarboxylic acid of the general formula X-Ala-Y-OR, where X is Ala, Leu, Phe, Ac-Tyr, Gly-Pro, Ac-Leu-Lys or Ac- Leu-Arg, Y is Acb, Acp or Ach, and R is methyl or ethyl, have been prepared. These peptides containing a rationally chosen N-substituent are cleaved with a suitable enzyme ( leucinaminopeptidase, alaninaminopeptidase, chymotrypsin, plasmin or kallikrein) in an ...