Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 17, Issue 7, Pages 2733-2743Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2009.02.038
Keywords
Glucokinase; Glucokinase activators; 3-Alkoxy-5-phenoxy-N-thiazolyl benzamides; Glucose-lowering effect
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Identification and synthesis of novel 3-alkoxy-5-phenoxy-N-thiazolyl benzamides as glucokinase activators are described. Removal of an aniline structure of the prototype lead (2a) and incorporation of an alkoxy or phenoxy substituent led to the identification of 3-Isopropoxy-5-[4-(methylsulfonyl) phenoxy]-N(4- methyl-1,3-thiazol-2-yl) benzamide (27e) as a novel, potent, and orally bioavailable GK activator. Rat oral glucose tolerance test indicated that 27e exhibited a glucose-lowering effect after 10 mg/kg oral administration. (c) 2009 Elsevier Ltd. All rights reserved.
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