Synthesis and biological evaluation of phosphonated dihydroisoxazole nucleosides Original Research Article

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.