Synthesis of Artificial Glycoconjugates of Arginine-Vasopressin and Their Antidiuretic Activities

Abstract

Arginine-vasopressin (AVP) derivatives modified at the glutamine side chain amide with carbohydrate via an alkylene spacer (la—d) were synthesized from new glycosylated glutamine derivatives (3a—d) by solid-phase synthesis. Glycoconjugates of AVP modified at the C-terminal amide (2a—d) were also synthesized from vasopressionic acid. All of them exhibited antidiuretic activity. © 1994, The Pharmaceutical Society of Japan. All rights reserved.