Abstract:
Novel peptides of ACTH activity, having a complete ACTH sequence from the N-terminal amino acid at least to the sixteenth amino acid, but containing optionally other amino acids in the place of the individual amino acids of the ACTH sequence, and always containing an Alpha -aminooxy acid in the place of the first amino acid have been prepared by deblocking the appropriate protected peptide derivatives. The new compounds, as well as their acid addition salts, derivatives or complexes possess potent ACTH activities and are resistant to enzymatic decomposition. They can be used in therapy with great advantages.
Abstract:
NEW N-ACYLATED HYDROXYLAMINE DERIVATIVES OF THE FORMULA
AC-NH-O-X
WHEREIN AC IS AN ACYL GROUP OF A CARBOXYLIC ACID CONTAINING ONE OR MORE BASIC NITROGEN ATOMS WITH THE EXCEPTION OF THE ALIPHATIC AMINO ACIDS LEUCINE, VALINE AND ALANINE AND X IS AN ARALKYL GROUP UNSUBSTITUTED OR SUBSTITUTED BY HALOGEN, LOWER ALKYL, LOWER ALKOXY OR THE NITRO GROUP, AND THE PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF, HAVING HYPOTENSIVE AND SEDATIVE EFFECT. THE NEW COMPOUNDS ARE PREPARED BY N-ACYLATIG AN /-SUBSTITUTED HYDROXYLAMINE OF THE FORMULA H2N-OX WITH THE CORRESPONDING AMINO ACID OR A REACTIVE DERIVATIVE THEREOF OR BY O-ARALKYLATING N- ACYLATED HYDROXYLAMINES