Abstract

9-[2-(Phosphonomethoxy)alkoxy]purines have been prepared and evaluated as antiviral agents. These compounds are the first reported acyclonucleotides in which an acyclic phosphonic acid-bearing substituent is attached to N-9 of a purine via a nitrogen-oxygen bond. Some 2-(phosphonomethoxy)ethoxy derivatives, e.g. (24), (25) and (27), have potent activity against herpesviruses. Some 3-hydroxy-2-(phosphonomethoxy)propoxy derivatives, e.g. (23) and (34), and a cyclic phosphonate (35), are potent and selective inhibitors of the replication of visna virus, a retrovirus.

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