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Small molecule ago-allosteric modulators of the human glucagon-like peptide-1 (hGLP-1) receptor. 2007
Min Teng, and
Michael D Johnson, and
Christine Thomas, and
Dan Kiel, and
James N Lakis, and
Tim Kercher, and
Shelley Aytes, and
Jarek Kostrowicki, and
Dilip Bhumralkar, and
Larry Truesdale, and
John May, and
Ulla Sidelman, and
Janos T Kodra, and
Anker Steen Jørgensen, and
Preben Houlberg Olesen, and
Johannes Cornelis de Jong, and
Peter Madsen, and
Carsten Behrens, and
Ingrid Pettersson, and
Lotte Bjerre Knudsen, and
Jens J Holst, and
Jesper Lau
Department of Medicinal Chemistry, Pfizer Global Research and Development, La Jolla, 10770 Science Center Dr., San Diego, CA 92121-1194, USA. min.teng@pfizer.com
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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