To obtain the subject new peptide derivative having a specific amino acid sequence containing phosphinic bonds, useful as a strongly selective inhibitor to endopeptidase 24-15, not acting on other zinc peptidases, and used for therapy of Alzheimer's disease, cancer, etc., and for other purposes.
This new peptide derivative having formula I [Ψ(PO2CH2) indicates that a peptide bond (CONH) is substituted by the phosphinic bonds (PO2CH2); Xaa' and Zaa' are each a natural amino acid or an amino pseudo acid; Yaa' is Arg or Lys]. The peptide derivative is a strongly selective inhibitor to zinc endopeptidase 24-15, does not act on the zinc peptidases, e.g. endopeptidase 24-16, a hypertensive converting enzyme, endopeptidase 24-11, aminopeptidases M and L, carboxypeptidases A and B, etc., and is useful for the therapy of Alzheimer's disease, cancer, hypertension, etc., and for other purposes. The compound is obtained by coupling the compound of formula II (R2 is a solid phase) to the compound of formula III (Z is acetyl, etc.; R3 is adamantyl) and subsequently removing R2 and R3 from the product.
JIRI JIRASETSUKU
ASANASHIOSU IOTAKISU
