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ID: ALA1140467
Journal: Bioorg Med Chem Lett
Title: Small molecule ago-allosteric modulators of the human glucagon-like peptide-1 (hGLP-1) receptor.
Authors: Teng M, Johnson MD, Thomas C, Kiel D, Lakis JN, Kercher T, Aytes S, Kostrowicki J, Bhumralkar D, Truesdale L, May J, Sidelman U, Kodra JT, Jørgensen AS, Olesen PH, de Jong JC, Madsen P, Behrens C, Pettersson I, Knudsen LB, Holst JJ, Lau J.
Abstract: Following our previous publication describing the biological profiles, we herein describe the structure-activity relationships of a core set of quinoxalines as the hGLP-1 receptor agonists. The most potent and efficacious compounds are 6,7-dichloroquinoxalines bearing an alkyl sulfonyl group at the C-2 position and a secondary alkyl amino group at the C-3 position. These findings serve as a valuable starting point for the discovery of more drug-like small molecule agonists for the hGLP-1 receptor.
CiteXplore: 17827014