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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
Authors:Antoinette Chougnet Prof.  Wolf‐D. Woggon Prof.  Esther Locher  Boris Schilling Dr.
Affiliation:1. Department of Chemistry, University of Basel, St.‐Johanns‐Ring 19, 4052 Basel (Switzerland);2. Givaudan Schweiz AG, Fragrance Research, Ueberlandstrasse 138, 8600 Duebendorf (Switzerland), Fax: (+41)?44‐824‐29‐26
Abstract:To be sniffed at : Several 1‐ and 2‐substituted 1H‐imidazoles and 2‐substituted oxazoles, oxazolines and pyrazines have been synthesized and tested as inhibitors of the cytochrome P450 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 μM .
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Keywords:CYP2A13  CYP2A6  cytochromes  inhibitors  respiratory tract
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