Synthesis and biological evaluation of glucagon-like peptide-1 receptor agonists

Yu Juan Zhang, Liu Lan Shen, Hyae Gyeong Cheon, Yong Nan Xu, Jin Hyun Jeong

Research output: Contribution to journalArticlepeer-review

8 Citations (Scopus)


In this study, a series of fused-heterocyclic derivatives were systematically designed and synthesized using an efficient route, and evaluated in terms of GLP-1R agonist activity. We employed short synthetic steps and reactions that are tolerant of the presence of various functional groups and suitable for parallel operations to enable the rapid generation of libraries of diverse and structurally complex small molecules. Of the compounds synthesized, 3-(8-chloro-6-(trifluoromethyl)imidazo[1,2-a] pyridin-2-yl)phenyl methanesulfonate (8e) was the most potent agonist with an EC50 of 7.89 μM, and thus is the compound with the greatest potential for application. These findings represent a valuable starting point for the design and discovery of small-molecule GLP-1R agonists that can be administered orally.

Original languageEnglish
Pages (from-to)588-599
Number of pages12
JournalArchives of pharmacal research
Issue number5
Publication statusPublished - 2014 May

Bibliographical note

Funding Information:
Acknowledgments This work was supported by the National Research Foundation of Korea (NRF) grant funded by the Korea government (MEST) (No. 2011-000-7061).

All Science Journal Classification (ASJC) codes

  • Molecular Medicine
  • Drug Discovery
  • Organic Chemistry


Dive into the research topics of 'Synthesis and biological evaluation of glucagon-like peptide-1 receptor agonists'. Together they form a unique fingerprint.

Cite this