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Peer-reviewed veterinary case report

Design, synthesis and SAR of novel glucokinase activators.

Journal:
Bioorganic & medicinal chemistry letters
Year:
2013
Authors:
Cheruvallath, Zacharia S et al.
Affiliation:
Takeda California · United States

Abstract

Guided by co-crystal structures of compounds 15, 22 and 30, an SBDD approach led to the discovery of the 6-methyl pyridone series as a novel class of GKAs that potently activate GK in enzyme and cell assays. Anti-diabetic OGTT efficacy was demonstrated with 54 in a mouse model of type 2 diabetes.

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Original publication: https://pubmed.ncbi.nlm.nih.gov/23434031/