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Synthesis of new 1-[2-Azido-2-(2,4-dichlorophenyl)ethyl]-1H/-imidazoles and in vitro evaluation of their antifungal activity
Authors:Francis Chevreuil  Anne Landreau  Gérald Larcher  Jean-Philippe Bouchara  Pascal Richomme
Affiliation:1. EA 921, Laboratoire SONAS, UFR des Sciences Pharmaceutiques et Ingénierie de la Santé16 Bd Daviers, 49100 Angers, France;2. IFR 149 Groupe d'Etude des Interactions H?te-Pathogène, CHU, 4 rue Larrey, 49933 Angers Cedex 9, France
Abstract:
New 1-[2-azido-2-(2,4-dichlorophenyl)ethyl]-1H/-imidazole were synthesized by nucleophilic substitution of various tertiary alcohols with azide anion in presence of boron trifluoride-diethyl etherate. Their antifungal activity was evaluated against Candida albicans, Candida glabrata, Aspergillus fumigatus and an azole-resistant petite mutant of C. glabrata. Preliminary SAR results are discussed.
Keywords:Antifungal agents  Candida albicans  Candida glabrata  conazole  azide  resistance  Aspergillus fumigatus
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