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Carbohydr Res. 2009 May 12;344(7):841-50. doi: 10.1016/j.carres.2009.02.012. Epub 2009 Feb 14.

Synthesis of glucoconjugates of oleanolic acid as inhibitors of glycogen phosphorylase.

Author information

1
PPSM, ENS Cachan, CNRS, UniverSud, 61 av President Wilson, F-94230 CACHAN, France.

Abstract

Synthesis and biological evaluation of glucoconjugates of oleanolic acid, linked by either a triazole moiety or an ester function, as novel inhibitors of glycogen phosphorylase have been described. Several triterpene-glycoside conjugates exhibited moderate-to-good inhibitory activity against rabbit muscle GPa. Compound 12 showed the best inhibition with an IC(50) value of 1.14 microM. Structure-activity relationship (SAR) analysis of these inhibitors is also discussed. Possible binding modes of compound 12 were explored by molecular docking simulations.

PMID:
19269628
DOI:
10.1016/j.carres.2009.02.012
[Indexed for MEDLINE]

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