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Issue 5, 2013
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N-substituted sultam carboxylic acids as novel glycogen synthase activators

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Abstract

Decreased glycogen synthesis and turnover is a common defect in type 2 diabetic patients. Activating glycogen synthase, the enzyme that catalyses the transfer of glucose from UDP-glucose to a glycogen polymer chain, could be a potential therapeutic target for the treatment of diabetes. We discovered a series of N-substituted sultam carboxylic acids as potent glycogen synthase activators. Treatment of human skeletal muscle cells with these compounds resulted in an increase in glycogen synthesis. Compound 4 displayed good oral bioavailability and therefore may be a useful tool molecule to study GS as a potential anti-diabetic target.

Graphical abstract: N-substituted sultam carboxylic acids as novel glycogen synthase activators

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Publication details

The article was received on 15 Feb 2013, accepted on 12 Mar 2013 and first published on 12 Mar 2013


Article type: Concise Article
DOI: 10.1039/C3MD00053B
Citation: Med. Chem. Commun., 2013,4, 833-838

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    N-substituted sultam carboxylic acids as novel glycogen synthase activators

    Y. Qian, D. R. Bolin, K. Conde-Knape, P. Gillespie, S. Hayden, K. Huang, M. Liu, A. R. Olivier, Y. Ren, J. Sergi, Q. Xiang, L. Yi, W. Yun and X. Zhang, Med. Chem. Commun., 2013, 4, 833
    DOI: 10.1039/C3MD00053B

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