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Synthesis and in vitro activity of heterocyclic inhibitors of CYP2A6 and CYP2A13, two cytochrome P450 enzymes present in the respiratory tract

Chougnet, Antoinette and Woggon, Wolf-D. and Locher, Esther and Schilling, Boris. (2009) Synthesis and in vitro activity of heterocyclic inhibitors of CYP2A6 and CYP2A13, two cytochrome P450 enzymes present in the respiratory tract. ChemBioChem, Vol. 10, H. 9. pp. 1562-1567.

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Official URL: http://edoc.unibas.ch/dok/A5260118

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Abstract

Several 1- and 2-substituted 1H-imidazoles and 2-substituted oxazoles, oxazolines and pyrazines have been synthesized and tested as inhibitors of the cytochrome P 450 enzymes CYP2A6 and CYP2A13.  1-Substituted 1H-imidazoles bearing short chains (pentyl, hexyl or hexenyl) were found to be potent inhibitors of both enzymes, and showed IC50 values of about 2 microM.  The synthesis of several heterocyclic compds. (1- or 2-substituted 1H-imidazoles and 2-substituted oxazoles, oxazolines and pyrazines) has been achieved.  These compds. were tested as inhibitors of CYP2A6 and CYP2A13-two cytochrome P 450 enzymes present in the respiratory tract-with a view to preventing the formation of carcinogenic metabolites of nicotine and inhibiting the metab. of fragrances. 1-Substituted imidazoles bearing short alkyl chains displayed IC50 values of around 2 microM for both enzymes, together with high vapor pressures.
Faculties and Departments:05 Faculty of Science
05 Faculty of Science > Departement Chemie > Chemie
UniBasel Contributors:Woggon, Wolf-Dietrich
Item Type:Article, refereed
Article Subtype:Research Article
Bibsysno:Link to catalogue
Publisher:Wiley-VCH
ISSN:1439-4227
Note:Publication type according to Uni Basel Research Database: Journal article
Last Modified:22 Mar 2012 14:25
Deposited On:22 Mar 2012 13:43

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