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    J Enzyme Inhib Med Chem. 2007 Oct;22(5):563-9.

    Synthesis of new isoxazoles and dihydroisoxazoles and in vitro evaluation of their antifungal activity.

    Source

    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.

    PMID:
    18035824
    [PubMed - indexed for MEDLINE]

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