Ethacrynic acid as a lead structure for the development of potent urease inhibitors |
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Authors: | Ingo Janser Caitlyn M. Vortolomei Ranjith K. Meka Courtney A. Walsh Romy F.J. Janser |
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Affiliation: | 1. Department of Chemistry, Eastern Michigan University, 48197 Ypsilanti, MI, USA;2. Department of Chemistry, New Mexico Institute of Mining and Technology, 87801 Socorro, NM, USA |
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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. |
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Keywords: | α,β-unsaturated ketones Ethacrynic acid Inhibitor Peptic ulcer Urease |
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