| Literature DB >> 23089526 |
Jeffrey A Pfefferkorn1, Meihua Tu, Kevin J Filipski, Angel Guzman-Perez, Jianwei Bian, Gary E Aspnes, Matthew F Sammons, Wei Song, Jian-Cheng Li, Christopher S Jones, Leena Patel, Tim Rasmusson, Dongxiang Zeng, Kapil Karki, Michael Hamilton, Richard Hank, Karen Atkinson, John Litchfield, Robert Aiello, Levenia Baker, Nicole Barucci, Patricia Bourassa, Francis Bourbonais, Francis Bourbounais, Theresa D'Aquila, David R Derksen, Margit MacDougall, Alan Robertson.
Abstract
Glucokinase activators represent a promising potential treatment for patients with Type 2 diabetes. Herein, we report the identification and optimization of a series of novel indazole and pyrazolopyridine based activators leading to the identification of 4-(6-(azetidine-1-carbonyl)-5-fluoropyridin-3-yloxy)-2-ethyl-N-(5-methylpyrazin-2-yl)-2H-indazole-6-carboxamide (42) as a potent activator with favorable preclinical pharmacokinetic properties and in vivo efficacy.Entities:
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Year: 2012 PMID： 23089526 DOI： 10.1016/j.bmcl.2012.09.082
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823