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Accueil > Recherche > Publications / brevets > Publications équipe SMALL > Synthèse valo biomolécules

Synthesis of Oleanolic Acid Dimers as Inhibitors of Glycogen Phosphorylase

K. G. Cheng, J. Liu, H. B. Sun and J. Xie Chem. Biodivers., 2010, 7 (3), 690-697

Références :

Chem. Biodivers., 2010, 7 (3), 690-697

Auteur(s) : 

K. G. Cheng, J. Liu, H. B. Sun and J. Xie

Recently, oleanolic acid was found to be an inhibitor of glycogen phosphorylase. For further structural modification, we have synthesized several dimers of oleanolic acid by using amide, ester, or triazole linkage with click chemistry. The click chemistry was shown to be the most efficient method for the dimer synthesis. Nearly quantitative yield of triazole-linked dimers was obtained. Biological evaluation of the synthesized dimers as inhibitors of glycogen phosphorylase has been described. Four of six dimers exhibited inhibitory activity against rabbit muscle glycogen phosphorylase a (RMGPa), with compounds 2 and 7 as the most potent inhibitors, which displayed an IC50 value (ca. 3 mu M) lower than that of oleanolic acid (IC50=14 mu M).

Type :
Publication
Dates :
Paru le 15 mars 2010
Informations complémentaires :
DOI: 10.1002/cbdv.200900086

 

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