Synthesis and preliminary anti-diabetic activity evaluation of novel PEGylated GLP-1 receptor agonists
10.11665/j.issn.1000-5048.20180507
- VernacularTitle:新型PEG化GLP-1受体激动剂的合成及其降血糖活性
- Author:
Yan LIU
1
;
Chengye LI
;
Xingguang CAI
;
Lidan SUN
;
Wenlong HUANG
Author Information
1. 重庆医科大学药学院
- Publication Type:Journal Article
- Keywords:
glucagon-like peptide-1;
derivatives;
PEG;
synthesis;
anti-diabetes activity
- From:
Journal of China Pharmaceutical University
2018;49(5):558-567
- CountryChina
- Language:Chinese
-
Abstract:
In order to obtain glucagon-like peptide-1(GLP-1)analogs which can sustainedly control the levels of glucose, 12 derivatives were designed and synthesized by coupling monomethoxy polyethylene glycol(mPEG, with average molecular weights of 350, 550 and 750)to GLP-1 analogs. Preliminary pharmacological activities showed that all compounds retained GLP-1 receptor agonist activities, and the hypoglycemic activity of compound I-12 was similar to those of Ex-4 and Liraglutide, suggesting I-12 could be a potential long-acting GLP-1 receptor agonist.
