5-Alkyl-2-urea-Substituted Pyridines: Identification of Efficacious Glucokinase Activators with Improved Properties

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• 作者：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 Jr. ; Christopher F. Kraser ; Ronald J. Hinklin ; Mark L. Boys ; Julio C. Medina ; Jonathan Houze ; Paul Dransfield ; Peter Coward
• 刊名：ACS Medicinal Chemistry Letters
• 出版年：2016
• 出版时间：July 14, 2016
• 年：2016
• 卷：7
• 期：7
• 页码：666-670
• 全文大小：365K
• 年卷期：0
• ISSN：1948-5875

文摘

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.