Abstract

Abstract: Nucleosides of 5-membered heterocycles are playing a prominent role in the design of antiviral agents. Included in this group is 4- hydroxy-3-( -D-ribofuranosyl)pyrazole-5-carboxamide (pyrazofurin), which is a naturally occurring C-nucleoside that shows significant broad spectrum in vitro antiviral activity against DNA and RNA viruses. The extent of its antiviral properties is represented by its activity against pox-, picorna, toga-, myxo-, rhabdo-, arena-, and bunyaviruses with a high degree of selectivity. Even with its promising activity and broad safety margin in cell cultures, there have been reports that the toxicity of pyrazo­ furin may limit its usefulness as an antiviral agent. However, others have suggested that the toxicity of pyrazofurin is unlikely to be associated with the structural components that are responsible for its antiviral properties. To evaluate this suggestion for the purpose of producing non-toxic pyrazofurin-derived agents that are effective against the virus groups mentioned above, structural modifications in pyrazofurin have recently been the subject of work in this laboratory. These efforts are described.

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