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Bioorg Med Chem Lett. 2007 Oct 1;17(19):5472-8. Epub 2007 Jul 4.

Small molecule ago-allosteric modulators of the human glucagon-like peptide-1 (hGLP-1) receptor.

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Department of Medicinal Chemistry, Pfizer Global Research and Development, La Jolla, 10770 Science Center Dr., San Diego, CA 92121-1194, USA.


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.

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