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

Varga, Gergely and Docsa, Tibor and Gergely, Pál and Juhász, László and Somsák, László (2013) Synthesis of tartaric acid analogues of FR258900 and their evaluation as glycogen phosphorylase inhibitors. Bioorganic & medicinal chemistry letters, 23 (6). pp. 1789-92. ISSN 1464-3405

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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).

Item Type: Article
Subjects: R Medicine / orvostudomány > RS Pharmacy and materia medica / gyógyszerészet, gyógyászati eszközök
Depositing User: Dr. Tibor Docsa
Date Deposited: 28 Sep 2015 02:23
Last Modified: 28 Sep 2015 02:23
URI: http://real.mtak.hu/id/eprint/28655

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