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Improved gelatinase a selectivity by novel zinc binding groups containing galardin derivatives
Franck Augé1, William Hornebeck, Martine Decarme
1UMR 6013 'Isolement, Structure, Transformation et Synthèse de Produits Naturelles', Faculté de Pharmacie, IFR53 Biomolécules, Université de Reims Champagne-Ardenne, 51 Rue Cognacq Jay, France.
Bioorganic & Medicinal Chemistry Letters
|May 6, 2003
Abstract:
The synthesis of several analogues of galardin, a MMP inhibitor, are presented with their in vitro inhibitory activity against MMP-1 and MMP-2. These compounds contain a distinct Zinc Binding Group (ZBG). Those having a 2-acylated-heterocycle as well as a 2-arylamide function do not exhibit a good inhibition/selectivity against the enzymes tested. On the contrary, those that are based on a hydrazide scaffold present potent selectivity for MMP-2 versus MMP-1.