Synthesis and antifungal activity of novel (1-aryl-2-heterocyclyl)ethylideneaminooxymethyl-substituted dioxolanes

A novel series of (1-aryl-2-heterocyclyl)ethylideneaminooxymethyl-substituted dioxolanes IIIa-n were synthesized by condensation of substituted 1,3-dioxolan-4-ylmethyl p-toluenesulfonates 4 with l-(hydroxyimino)-1-aryl-2-heterocyclylethanes 5. Compounds IIIa-n were found to have effective in vitro a...

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Bibliographic Details
Published in:European journal of medicinal chemistry 1995, Vol.30 (7), p.617-626
Main Authors: Baji, H, Flammang, M, Kimny, T, Gasquez, F, Compagnon, PL, Delcourt, A
Format: Article
Language:English
Subjects:
1,2,4-triazole
1,3-dioxolane
antifungal activity
ethylideneaminooxy
imidazole
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Summary:A novel series of (1-aryl-2-heterocyclyl)ethylideneaminooxymethyl-substituted dioxolanes IIIa-n were synthesized by condensation of substituted 1,3-dioxolan-4-ylmethyl p-toluenesulfonates 4 with l-(hydroxyimino)-1-aryl-2-heterocyclylethanes 5. Compounds IIIa-n were found to have effective in vitro antifungal activity when evaluated against the pathogenic fungi Candida albicans, Aspergillus flavus and Fusarium solani with MIC (minimum inhibitory concentration) values of 10 μg·ml −1 for IIIa-1 and 5 μg·ml −1 for IIIm,n.
ISSN:0223-5234
1768-3254
DOI:10.1016/0223-5234(96)88277-8