Journal
LIFE SCIENCES
Volume 73, Issue 23, Pages 2985-2990Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/S0024-3205(03)00708-2
Keywords
alpha,beta-unsaturated ketones; urease inhibitor; Jack bean urease
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A variety of alpha,beta-unsaturated ketones were evaluated for their effect on the jack bean urease. Of 35 compounds tested, 2-cyclohepten-1-one (1), 2-cyclohexen-1-one (2), 2-cyclopenten-1-one (3), and 5,6-dihydro-2H-pyran-2-one (4) showed potent inhibitory activities against the enzyme. The most potent compound (1) (IC50 = 0.16 mM) showed similar inhibitory potency to hydroxyurea (IC50 = 0.095 mM). The inhibitory effects of 1, 2, 3, and 4 were significantly reduced by 2-mercaptoethanol or dithiothreitol. These data suggest that alpha,beta-unsaturated ketones inhibited the urease activity, possibly by a Michael-like addition of a protein SH group to the double bond of the alpha,beta-unsaturated carbonyl group. (C) 2003 Elsevier Inc. All rights reserved.
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