Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1379056 | Bioorganic & Medicinal Chemistry Letters | 2006 | 4 Pages |
Inhibitory activity of organobismuth compounds, triarylbismuthanes 1 and their dihalides 2 and 3, was examined against jack bean urease. Besides triarylbismuth dichlorides 2, triarylbismuth difluorides 3 and bismuthanes 1 exhibited the activity. Of all these compounds, triphenylbismuth difluoride 3a and tris(4-fluorophenyl)bismuth dichloride 2b showed the highest activity. These results indicate that generation of the inhibitory effect is not always governed by the Lewis acidity at the bismuth center. Such a tendency of inhibition by the organobismuth compounds is in good accord with that observed in the antibacterial activity against Helicobacter pylori, suggesting that H. pylori-produced urease may be a therapeutic target by bismuth-based drugs.
Graphical abstractInhibitory activity of organobismuth compounds was tested against jack bean urease. Triphenylbismuth difluoride showed the highest activity. The tendency of the inhibition is in good agreement with that observed in the antibacterial activity against Helicobacter pylori.Figure optionsDownload full-size imageDownload as PowerPoint slide