Inhibition of jack bean urease by organobismuth compounds

Inhibitory 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. Inhibitory activity of organo...

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Bibliographic Details
Published in:	Bioorganic & medicinal chemistry letters Vol. 16; no. 6; pp. 1510 - 1513
Main Authors:	Murafuji, Toshihiro, Azuma, Takako, Miyoshi, Youhei, Ishibashi, Motoko, Rahman, A.F.M. Mustafizur, Migita, Kouto, Sugihara, Yoshikazu, Mikata, Yuji
Format:	Journal Article
Language:	English
Published:	Oxford Elsevier Ltd 15-03-2006 Elsevier
Subjects:	Antibacterial agents Antibiotics. Antiinfectious agents. Antiparasitic agents Antifungal Agents - chemistry Antifungal Agents - pharmacology Biological and medical sciences Bismuth Bismuth - chemistry Bismuth - pharmacology Fabaceae - enzymology Helicobacter Infections - drug therapy Helicobacter pylori Helicobacter pylori - enzymology Jack bean urease Medical sciences Microbial Sensitivity Tests Molecular Structure Organobismuth Organometallic Compounds - chemical synthesis Organometallic Compounds - chemistry Organometallic Compounds - pharmacology Pharmacology. Drug treatments Saccharomyces cerevisiae - drug effects Saccharomyces cerevisiae - growth & development Structure-Activity Relationship Urease - antagonists & inhibitors Urease - metabolism Urease inhibitor Bismuth Organobismuth Urease inhibitor Helicobacter pylori Jack bean urease Canavalia ensiformis Molecular structure Spirillaceae Antiulcer agent Structure activity relation Dicotyledones Angiospermae Bacteria Spirillales Enzyme Benzene derivatives Enzyme inhibitor Urease X ray diffraction In vitro Grain legume Leguminosae Bismuth Organic compounds Hydrolases Spermatophyta Models Kinetics Antibacterial agent Crystalline structure
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Summary:	Inhibitory 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. 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.
Bibliography:	ObjectType-Article-1 SourceType-Scholarly Journals-1 ObjectType-Feature-2 content type line 23
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2005.12.034