Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594352 | Bioorganic & Medicinal Chemistry Letters | 2012 | 6 Pages |
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.
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Authors
Jeffrey A. Pfefferkorn, 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,