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Design,Synthesis, Antiviral,and Cytostatic Evaluation of Novel Isoxazolidine Analogues of C-Nucleotides
Authors:Magdalena Grabkowska-Drużyc  Jan Balzarini  Dorota G Piotrowska
Institution:1. Bioorganic Chemistry Laboratory, Faculty of Pharmacy , Medical University of ?ód? , ?ód? , Poland;2. Rega Institute for Medical Research , KU Leuven , Belgium
Abstract:5-Aryl-2-methylisoxazolidin-3-yl-3-phosphonates have been synthesised from N-methyl-C-diethoxyphosphorylnitrone and vinyl aryls in good yields. Isoxazolidine phosphonates obtained herein were evaluated for activity against a broad range of DNA and RNA viruses. None of the compounds were endowed with antiviral activity nor cytostatic activity at 100 to 250 μM concentrations.
Keywords:C-nucleotide analogues  phosphonates  isoxazolidines  1  3-dipolar cycloaddition
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