Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 17, Issue 11, Pages 3800-3809Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.04.040
Keywords
Glucokinase; Glucokinase activator; 3,5-Disubstituted benzamides; Glucose lowering efficacy; Log D
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The optimization of our lead GK activator 2a to 3-[(1S)-2-hydroxy-1-methylethoxy]-5-[4-(methylsulfonyl) phenoxy]-N-1,3-thiazol-2-ylbenzamide (6g), a potent GK activator with good oral availability, is described, including to uncouple the relationship between potency and hydrophobicity. Following oral administration, this compound exhibited robust glucose lowering in diabetic model rodents. (C) 2009 Elsevier Ltd. All rights reserved.
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