Source:http://linkedlifedata.com/resource/pubmed/id/14519447
Switch to
| Predicate | Object |
|---|---|
| rdf:type | |
| lifeskim:mentions | |
| pubmed:issue |
23
|
| pubmed:dateCreated |
2003-10-1
|
| pubmed:abstractText |
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.
|
| pubmed:language |
eng
|
| pubmed:journal | |
| pubmed:citationSubset |
IM
|
| pubmed:chemical | |
| pubmed:status |
MEDLINE
|
| pubmed:month |
Oct
|
| pubmed:issn |
0024-3205
|
| pubmed:author | |
| pubmed:issnType |
Print
|
| pubmed:day |
24
|
| pubmed:volume |
73
|
| pubmed:owner |
NLM
|
| pubmed:authorsComplete |
Y
|
| pubmed:pagination |
2985-90
|
| pubmed:meshHeading |
pubmed-meshheading:14519447-Enzyme Inhibitors,
pubmed-meshheading:14519447-Fabaceae,
pubmed-meshheading:14519447-Hydroxyurea,
pubmed-meshheading:14519447-Inhibitory Concentration 50,
pubmed-meshheading:14519447-Ketones,
pubmed-meshheading:14519447-Structure-Activity Relationship,
pubmed-meshheading:14519447-Urease
|
| pubmed:year |
2003
|
| pubmed:articleTitle |
Urease inhibitory activity of simple alpha,beta-unsaturated ketones.
|
| pubmed:affiliation |
Faculty of Pharmaceutical Sciences, Josai University, Sakado, Saitama 350-0295, Japan.
|
| pubmed:publicationType |
Journal Article
|