Discovery of a novel potent GPR40 full agonist

Bioorganic & Medicinal Chemistry Letters
2018.0

Abstract

Compound 12 is a GPR40 agonist that realizes the full magnitude of efficacy possible via GPR40 receptor agonism. In vitro and in vivo studies demonstrated superior glucose lowering by 12 compared to fasiglifam (TAK-875), in a glucose dependent manner. The enhanced efficacy observed with the full agonist 12 was associated with both direct and indirect stimulation of insulin secretion.

Knowledge Graph

Similar Paper

Discovery of a novel potent GPR40 full agonist
Bioorganic & Medicinal Chemistry Letters 2018.0
The Discovery, Preclinical, and Early Clinical Development of Potent and Selective GPR40 Agonists for the Treatment of Type 2 Diabetes Mellitus (LY2881835, LY2922083, and LY2922470)
Journal of Medicinal Chemistry 2016.0
Discovery of N -arylpyrroles as agonists of GPR120 for the treatment of type II diabetes
Bioorganic & Medicinal Chemistry Letters 2018.0
Design, synthesis and biological evaluation of a series of novel GPR40 agonists containing nitrogen heterocyclic rings
Bioorganic & Medicinal Chemistry Letters 2018.0
Discovery of a Potent Free Fatty Acid 1 Receptor Agonist with Low Lipophilicity, Low Polar Surface Area, and Robust in Vivo Efficacy
Journal of Medicinal Chemistry 2016.0
Design, Synthesis, and Evaluation of Novel and Selective G-protein Coupled Receptor 120 (GPR120) Spirocyclic Agonists
ACS Medicinal Chemistry Letters 2017.0
Design, synthesis and biological evaluation of novel FFA1/GPR40 agonists: New breakthrough in an old scaffold
European Journal of Medicinal Chemistry 2019.0
Recent Updates on Free Fatty Acid Receptor 1 (GPR-40) Agonists for the Treatment of Type 2 Diabetes Mellitus
Mini-Reviews in Medicinal Chemistry 2021.0
Design, synthesis and structure–activity relationship studies of novel free fatty acid receptor 1 agonists bearing amide linker
Bioorganic & Medicinal Chemistry 2017.0
Novel free fatty acid receptor 1 (GPR40) agonists based on 1,3,4-thiadiazole-2-carboxamide scaffold
Bioorganic & Medicinal Chemistry 2016.0