Susaki H, Suzuki K, Ikeda M, Yamada H, Watanabe H K
Drug Delivery System Institute, Ltd., Chiba, Japan.
Chem Pharm Bull (Tokyo). 1994 Oct;42(10):2090-6. doi: 10.1248/cpb.42.2090.
Arginine-vasopressin (AVP) derivatives modified at the glutamine side chain amide with carbohydrate via an alkylene spacer (1a--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.
通过固相合成法，由新的糖基化谷氨酰胺衍生物（3a - d）合成了在谷氨酰胺侧链酰胺处通过亚烷基间隔基与碳水化合物修饰的精氨酸加压素（AVP）衍生物（1a - d）。还从加压素酸合成了在C末端酰胺处修饰的AVP糖缀合物（2a - d）。它们都表现出抗利尿活性。
