- 5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties.
5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties.
ACS medicinal chemistry letters (2016-07-21)
Todd J Kohn, Xiaohui Du, SuJen Lai, YuMei Xiong, Renee Komorowski, Murielle Veniant, Zice Fu, Xianyun Jiao, Vatee Pattaropong, David Chow, Mario Cardozo, Lixia Jin, Marion Conn, Walter E DeWolf, Christopher F Kraser, Ronald J Hinklin, Mark L Boys, Julio C Medina, Jonathan Houze, Paul Dransfield, Peter Coward
PMID27437074
摘要
Two 1-(4-aryl-5-alkyl-pyridin-2-yl)-3-methylurea glucokinase activators were identified with robust in vivo efficacy. These two compounds possessed higher solubilities than the previously identified triaryl compounds (i.e., AM-2394). Structure-activity relationship studies are presented along with relevant pharmacokinetic and in vivo data.
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