Synthesis,characterization and antifungal testing of 3,4-dihydropyrimidin-2(1H)-(thio)ones containing boronic acids and boronate esters |
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| Authors: | Dominique R Duguay Matthew T Zamora Johanna M Blacquiere Francis E Appoh Christopher M Vogels Susan L Wheaton Felix J Baerlocher Andreas Decken Stephen A Westcott |
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| Institution: | (1) Department of Chemistry, Mount Allison University, Sackville, NB, E4L 1G8, Canada;(2) Department of Biology, Mount Allison University, Sackville, NB, E4L 1G7, Canada;(3) Department of Chemistry, University of New Brunswick, Fredericton, NB, E3B 5A3, Canada |
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| Abstract: | The addition of formylphenylboronic acid derivatives to thiourea and ethyl acetoacetate proceeds in the presence of an additional
Lewis acid catalyst to give the corresponding 3,4-dihydropyrimidin-2(1H)-(thio)ones (Biginelli products) in moderate yield.
Compounds were tested for antifungal activity against pure cultures of Aspergillus niger, Aspergillus flavus, Candida albicans and Saccharomyces cerevisiae but, unfortunately, none showed any appreciable activity.
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| Keywords: | Antifungal Biginelli compounds Boron 3 4-dihydropyrimidin-2(1H)-(thio)ones Monastrol |
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