Synthesis and biological evaluation of phosphonated dihydroisoxazole nucleosides |
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Authors: | Romeo Giovanni Iannazzo Daniela Piperno Anna Romeo Roberto Saglimbeni Monica Chiacchio Maria Assunta Balestrieri Emanuela Macchi Beatrice Mastino Antonio |
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Institution: | Dipartimento Farmaco-Chimico, Università di Messina, Via SS. Annunziata, Messina 98168, Italy. gromeo@unime.it |
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Abstract: | Phosphonated isoxazolinyl nucleosides have been prepared via 1,3-dipolar cycloaddition reaction of nitrile oxides with corresponding vinyl or allyl nucleobases for antiviral studies. The cytotoxicity, the anti-HSV activity and the RT-inhibitory activity of the obtained compounds were evaluated and compared with those of AZT and diethyl{(1'SR,4'RS)-1'-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)]-3'-methyl-2'-oxa-3'-azacyclopent-4'-yl]}methylphosphonate, a saturated phosphonated dihydroisoxazole nucleoside analogue. |
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