Synthesis and Antiviral Evaluation of Pyrazofurin Analogues.

摘要

5'-Deoxypyrazofurin and N-methyl and N, N-dimethyl carboxamido derivatives of pyrazofurin have been prepared and submitted to the Army for antiviral analysis. Antiviral data for 4-deoxy- and 4-homopyrazofurin and their acyclo derivatives (synthesized during the previous year) has been received and the four compounds were found to be non-toxic and lacking any appreciable antiviral properties. Synthetic methods towards a number of target pyrazofurin derivatives have been evaluated. The derivatives sought have been: 5'-homopyrazofurin, pyrazofurin nor-amide, 2-deazapyrazofurin, 1-deazapyrazofurin, 5'-amino-5'-deoxypyrazofurin two phosphonate pyrazofurins, a phosphoramidite derivative of pyrazofurin 3'-fluoro-3'- deoxypyrazofurin, and 2'- and 3'-deoxypyrazofurin. These efforts have so far led to one paper having appeared in the professional literature, one paper accepted for publication, and one paper just submitted. During this reporting period, a supply of pyrazofurin was received from Eli Lilly Company that has been useful to this project.