Synthesis of new isoxazoles and dihydroisoxazoles and in vitro evaluation of their antifungal activity |
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Authors: | Chevreuil Francis Landreau Anne Séraphin Denis Larcher Gérald Mallet Sabine Bouchara Jean-Philippe Richomme Pascal |
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Affiliation: | Laboratoire SONAS, UPRES-EA 921, UFR des Sciences Pharmaceutiques, Angers, France. |
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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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