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Synthesis of new isoxazoles and dihydroisoxazoles and in vitro evaluation of their antifungal activity
Authors:Chevreuil Francis  Landreau Anne  Séraphin Denis  Larcher Gérald  Mallet Sabine  Bouchara Jean-Philippe  Richomme Pascal
Institution:Laboratoire SONAS, UPRES-EA 921, UFR des Sciences Pharmaceutiques, Angers, France.
Abstract:New 2-(2,4-dihalogenophenyl)-1-(1H-imidazol-1-yl)-3-(isoxazol-5-yl)propan-2-ols and 2-(2,4-dihalogenophenyl)-1-(1H-imidazol-1-yl)-3-(4,5-dihydroisoxazol-5-yl)propan-2-ols were synthesized by 1,3-dipolar cycloaddition between homopropargylic or homoallylic alcohols and in-situ generated nitrile oxide. Their antifungal activity was evaluated against Candida albicans, C. glabrata, Aspergillus fumigatus and an azole-resistant petite mutant of C. glabrata. Preliminary SAR results are discussed.
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