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

[Image: see text] 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 pres...

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Detalles Bibliográficos
Autores principales: Kohn, Todd J., Du, Xiaohui, Lai, SuJen, Xiong, YuMei, Komorowski, Renee, Veniant, Murielle, Fu, Zice, Jiao, Xianyun, Pattaropong, Vatee, Chow, David, Cardozo, Mario, Jin, Lixia, Conn, Marion, DeWolf, Walter E., Kraser, Christopher F., Hinklin, Ronald J., Boys, Mark L., Medina, Julio C., Houze, Jonathan, Dransfield, Paul, Coward, Peter
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2016
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4948010/
https://www.ncbi.nlm.nih.gov/pubmed/27437074
http://dx.doi.org/10.1021/acsmedchemlett.6b00145
Descripción
Sumario:[Image: see text] 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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