Ethacrynic acid as a lead structure for the development of potent urease inhibitors - 10/07/13
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Abstract |
Ethacrynic acid and a series of its analogues were synthesized and subsequently evaluated for their inhibitory effect on jack bean urease. Ethacrynic acid showed, even at low concentrations, very potent inhibitory activity against the enzyme. For ethacrynic acid, the inhibition potential increased with increasing preincubation time of ethacrynic acid and enzyme, whereas for some other compounds a higher preincubation time lead to a significant reduction of their activity. We could demonstrate that the α,β-unsaturated carbonyl unit of our compounds is mandatory to inhibit the enzyme, possibly due to its ability to bind to cysteine residues in the active site of the jack bean urease.
Le texte complet de cet article est disponible en PDF.Keywords : α,β-unsaturated ketones, Ethacrynic acid, Inhibitor, Peptic ulcer, Urease
Plan
Vol 16 - N° 7
P. 660-664 - juillet 2013 Retour au numéroBienvenue sur EM-consulte, la référence des professionnels de santé.
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