Dilip Dixit

STRUCTURE-ACTIVITY RELATIONSHIPS AMONG A NEW CLASS OF ANTIVIRAL HETEROSUBSTITUTED 2',3'-DIDEOXYNUCLEOSIDE ANALOGUES

Abstract 3′-Oxa-4′-thiocytidine nucleoside analogues 14–17 were prepared from oxathiolanes 10 and 11, and evaluated for activity against HIV-1 and HBV in vitro. The nucleoside analogues were found to possess potent activities against HIV-1 in a panel of cell lines. Compound 16 is moderately active against HBV in 2.2.15 cells.

Synthesis of 5-Substituted-1-[[2-Hydroxy-1-(hydroxymethyl)ethoxy]methyl]cytosines

Abstract 5-Substituted cytosine analogues of 9-[[2-hydroxy-1-(hydroxymethyl)ethoxy]methyl]guanine (BIOLF-62) have been synthesized and tested against HSV-1.

Synthesis of racemic 2-phosphonomethyl-1,3-dioxolane nucleoside analogues as potential antiviral agents

Abstract 2-Phosphonomethyl-1,3-dioxolane nucleosides containing appropriately linked pyrimidine and purine bases at C-4 position were prepared as biomimetic analogues of antiviral 2′,3′-dideoxynucleoside monophosphates. The key coupling intermediate 10 was prepared by a cyclocondensation of diethylacetal 6 and diol 7 followed by hydrolysis and lead tetra-acetate oxidative decarboxylation.