Design, synthesis, and biological activity of novel dicoumarol glucagon-like peptide 1 conjugates

J Han, L Sun, Y Chu, Z Li, D Huang, X Zhu…

Index: Han, Jing; Sun, Lidan; Chu, Yingying; Li, Zheng; Huang, Dandan; Zhu, Xiaoyun; Qian, Hai; Huang, Wenlong Journal of Medicinal Chemistry, 2013 , vol. 56, # 24 p. 9955 - 9968

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Citation Number: 10

Abstract

Twelve novel dicoumarol glucagon-like peptide 1 (GLP-1) conjugates were designed, synthesized, and tested for biological activity. All derivatives retained receptor activation efficacy, and exhibited improved albumin affinity and in vitro stability in rat plasma. The in vivo elimination half-lives of 13c and 13l (22.07 and 18.78 h, respectively) were much longer than those of the GLP-1 receptor agonists exendin-4 (2.82 h) and liraglutide (12.53 h). The ...