title: Inhibition of jack bean urease by organobismuth compounds.
abstract: 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.
authors.affiliation: Department of Chemistry, Faculty of Science, Yamaguchi University, Yamaguchi 753-8512, Japan. murafuji@yamaguchi-u.ac.jp
authors.forename: Toshihiro
authors.initials: T
authors.lastname: Murafuji
authors.forename: Takako
authors.initials: T
authors.lastname: Azuma
authors.forename: Youhei
authors.initials: Y
authors.lastname: Miyoshi
authors.forename: Motoko
authors.initials: M
authors.lastname: Ishibashi
authors.forename: A F M Mustafizur
authors.initials: AF
authors.lastname: Rahman
authors.forename: Kouto
authors.initials: K
authors.lastname: Migita
authors.forename: Yoshikazu
authors.initials: Y
authors.lastname: Sugihara
authors.forename: Yuji
authors.initials: Y
authors.lastname: Mikata
mesh_terms: D000935:Antifungal Agents / Q000737:chemistry / Q000494:pharmacology; D001729:Bismuth / Q000737:chemistry / Q000494:pharmacology*; D007887:Fabaceae / Q000201:enzymology*; D016481:Helicobacter Infections / Q000188:drug therapy; D016480:Helicobacter pylori / Q000201:enzymology; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D012441:Saccharomyces cerevisiae / Q000187:drug effects* / Q000254:growth & development; D013329:Structure-Activity Relationship; D014510:Urease / Q000037:antagonists & inhibitors* / Q000378:metabolism
chemical_list: D000935:Antifungal Agents; D009942:Organometallic Compounds; D014510:Urease; D001729:Bismuth