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Bioorg Med Chem Lett. 2013 Mar 15;23(6):1789-92. doi: 10.1016/j.bmcl.2013.01.042. Epub 2013 Jan 22.

Synthesis of tartaric acid analogues of FR258900 and their evaluation as glycogen phosphorylase inhibitors.

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1
Department of Organic Chemistry, Faculty of Science and Technology, University of Debrecen, PO Box 20, H-4010 Debrecen, Hungary.

Abstract

Di-O-cinnamoylated, -p-coumaroylated, and -feruloylated d-, l- and meso-tartaric acids were synthesized as analogues of the natural product FR258900, a glycogen phosphorylase (GP) inhibitor with in vivo antihyperglycaemic activity. The new compounds inhibited rabbit muscle GP in the low micromolar range, and bound to the allosteric site of the enzyme. The best inhibitor was 2,3-di-O-feruloyl meso-tartaric acid and had Ki values of 2.0μM against AMP (competitive) and 3.36μM against glucose-1-phosphate (non-competitive).

PMID:
23395662
DOI:
10.1016/j.bmcl.2013.01.042
[Indexed for MEDLINE]
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