Synthesis and biological evaluation of 1, 2, 4‐oxadiazole derivatives as novel GPR119 agonists
Copyright policy )Synthesis and biological evaluation of 1, 2, 4‐oxadiazole derivatives as novel GPR119 agonists
A series of 1, 2, 4‐oxadiazole derivatives have been designed and synthesized, and 25 compounds were evaluated their abilities by the assay of cAMP concentration in GPR119‐transfected HEK293T cells. All compounds showed acceptable agonistic effects on GPR119. Among these compounds, 4p exhibited the best agonistic effects with the EC50 of 20.6 nm, which was comparable to that of positive control GPR119 agonist GSK1292263. The agonistic activity of these 1,2,4‐oxadiazole derivatives led to the establishment of a structure–activity relationship.
- West China Hospital of Sichuan University China (People's Republic of)
- China Medical University China (People's Republic of)
- Sichuan University China (People's Republic of)
Mesylates, Oxadiazoles, Drug Evaluation, Preclinical, Receptors, G-Protein-Coupled, Structure-Activity Relationship, HEK293 Cells, Drug Design, Cyclic AMP, Humans, Hypoglycemic Agents, Protein Binding
Mesylates, Oxadiazoles, Drug Evaluation, Preclinical, Receptors, G-Protein-Coupled, Structure-Activity Relationship, HEK293 Cells, Drug Design, Cyclic AMP, Humans, Hypoglycemic Agents, Protein Binding
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