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Updated: Jul 11, 2026

Mechanisms Underlying Gut Hormone Secretion Using the Isolated Perfused Rat Small Intestine
Published on: February 26, 2019
Small molecule ago-allosteric modulators of the human glucagon-like peptide-1 (hGLP-1) receptor
Min Teng1, Michael D Johnson, Christine Thomas
1Department of Medicinal Chemistry, Pfizer Global Research and Development, La Jolla, 10770 Science Center Dr., San Diego, CA 92121-1194, USA. min.teng@pfizer.com
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.
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