Details

Autor(en) / Beteiligte

• Chen, Helen Y.
• Plummer, Christopher W.
• Xiao, Dong
• Chobanian, Harry R.
• DeMong, Duane
• Miller, Michael
• Trujillo, Maria E.
• Kirkland, Melissa
• Kosinski, Daniel
• Mane, Joel
• Pachanski, Michele
• Cheewatrakoolpong, Boonlert
• Di Salvo, Jerry
• Thomas-Fowlkes, Brande
• Souza, Sarah
• Tatosian, Daniel A.
• Chen, Qing
• Hafey, Michael J.
• Houle, Robert
• Nolting, Andrew F.
• Orr, Robert
• Ehrhart, Juliann
• Weinglass, Adam B.
• Tschirret-Guth, Richard
• Howard, Andrew D.
• Colletti, Steven L.

Titel

Structure–Activity Relationship of Novel and Selective Biaryl-Chroman GPR40 AgoPAMs

Ist Teil von

• ACS medicinal chemistry letters, 2018-07, Vol.9 (7), p.685-690

Ort / Verlag

United States: American Chemical Society

Erscheinungsjahr

2018

Quelle

Alma/SFX Local Collection

Beschreibungen/Notizen

• A series of biaryl chromans exhibiting potent and selective agonism for the GPR40 receptor with positive allosteric modulation of endogenous ligands (AgoPAM) were discovered as potential therapeutics for the treatment of type II diabetes. Optimization of physicochemical properties through modification of the pendant aryl rings resulted in the identification of compound AP5, which possesses an improved metabolic profile while demonstrating sustained glucose lowering.