Abstract

The synthesis of new cyclic and acyclic nucleoside analogues was achieved by alkylation of 5-halogenated 6-(2,4-dichlorophenoxymethyl)pyrimidine-2,4-dione following the Vorbruggen coupling procedure. Nucleoside analogues of the 1-[(2-hydroxy-ethoxy)methyl]-6-(phenylthio)thymine (HEPT)-type were obtained as well as analogues ofganciclovir, acyclovir, and ribonucleosides. All compounds were tested against a variety of viruses. Three of the new compounds were potent and selective anti-HIV-1 inhibitors.

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