The State University of New York

Alan C Schroeder

Yung-Chi Cheng

Thomas J Bardos

Simon M Efange

The nuceoside 1-(2-Deoxy-.beta.-D-ribofuranosyl)-5-(iodo)-2-pyrimidinone possesses a high level of antiviral activity and a low level of toxicity to the host cell making it an especially effective therapeutic agent for HSV-2.

5-ioso-2-pyrimidinone nucleoside

Compounds for inhibiting the replication of DNA viruses which induce the formation of thymidine kinase enzyme of the formula: ##STR1## wherein R.sub.1 is a radical selected from the group consisting of chloro, iodo, hydroxy, alkoxyalkyl, hydroxyalkyl, methylamino, formyl, nitro, and unsubstituted hydrocarbon groups of 2 to about 3 carbon atoms or halosubstituted hydrocarbon groups of 1 to about 3 carbon atoms; R.sub.2 is hydrogen or hydroxy; and R.sub.3 is hydroxy, --OP(O)(OH).sub.2, amino, or --OCOR.sub.4 where R.sub.4 is alkyl or alkoxyalkyl of 2 to about 18 carbon atoms.

Novel 5-substituted 2-pyrimidinone nucleosides and methods of use

A method for inhibiting the replication of a DNA virus which induces formation of thymidine kinase enzyme, by exposing the virus to an effective concentration of a compound of the formula: ##STR1## wherein R.sub.1 is a radical selected from the group consisting of halogen, --SCH.sub.3, --OH, alkoxy, cyano, methylamino, carboxy, formyl, nitro and unsubstituted or halosubstituted hydrocarbon groups of 1 through 3 carbon atoms; R.sub.2 is hydrogen; halogen or hydroxy; and R.sub.3 is hydroxy, --OP(O)(OH).sub.2, amino, or --OOR.sub.4 where R.sub.4 is lower alkyl of 1 through 6 carbon atoms.

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Silver Springs, MD, United States of America

Alan C Schroeder