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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
JournalArticle (Originalarbeit in einer wissenschaftlichen Zeitschrift)
 
ID 163211
Author(s) Chougnet, Antoinette; Woggon, Wolf-D; Locher, Esther; Schilling, Boris
Author(s) at UniBasel Woggon, Wolf-Dietrich
Year 2009
Title Synthesis and in vitro activity of heterocyclic inhibitors of CYP2A6 and CYP2A13, two cytochrome P450 enzymes present in the respiratory tract
Journal ChemBioChem
Volume 10
Number 9
Pages / Article-Number 1562-7
Keywords CYP2A13, CYP2A6, cytochromes, inhibitors, respiratory tract
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.

Publisher Wiley-VCH
ISSN/ISBN 1439-4227
edoc-URL http://edoc.unibas.ch/dok/A5260118
Full Text on edoc No
Digital Object Identifier DOI 10.1002/cbic.200800712
PubMed ID http://www.ncbi.nlm.nih.gov/pubmed/19434638
ISI-Number WOS:000267500400022
Document type (ISI) Article
 
   

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