CN
- Synthesis of tartaric acid analogues of FR258900 and their evaluation as glycogen phosphorylase inhibitors.
Synthesis of tartaric acid analogues of FR258900 and their evaluation as glycogen phosphorylase inhibitors.
Bioorganic & medicinal chemistry letters (2013-02-12)
Gergely Varga, Tibor Docsa, Pál Gergely, László Juhász, László Somsák
PMID23395662
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).
MATERIALS
Product Number
Brand
Product Description
Sigma-Aldrich
L-(+)-Tartaric acid, puriss., meets analytical specification of Ph. Eur., NF, 99.7-100.5% (calc. to the dried substance), powder
Supelco
L-(+)-Tartaric acid, certified reference material, TraceCERT®, Manufactured by: Sigma-Aldrich Production GmbH, Switzerland
Sigma-Aldrich
L-(+)-Tartaric acid, puriss. p.a., reag. ISO, 99.5-101.0% (calc. to the dried substance)