Analogues of Arginine Vasopressin(AVP)Modified in the N-terminal Part of the Molecule with Stereoisomers of 4-Aminopyroglutamic Acid

摘要

The present work is a part of our studies aimed at clarifying the influence of sterical constraints in N-terminal part of AVP analogues on the pharmacological activity of the resulting peptides.In this study we described the synthesis of four new analogues of AVP substituted at positions 2 and 3 or 3 and 4 with two diastereoisomers of 4-aminopyro-glutamic acid and four peptides in which we combined the above modification with the placement of 3-mercaptopropionic acid at position 1.All new peptides were not active in bioassays for pressor,antidiuretic and uterotonic activity.