Synthesis and Antiviral Evaluation of Pyrazofurin Analogues.
Abstract
4-Deoxypyrazofurin (2) and its acyclic derivative (3), 4-homopyrazofurin (4) and its acyclic derivative (5), N-methyl-(6) and N,N-dimethylpyrazofurin(7), 5'-deoxypyrazofurin (8), and 5'- homopyrazofurin (9) were prepared and evaluated as antiviral agents during this program. Other pyrazofurin derivatives sought but whose synthesis was riot achieved Were Pyrazofurin nor-amide (10), 5, -amino-5' -deoxypyrazofurin (11), 5'-deoxy-5'-phosphonylpyrazofurin (12), 5 '-deoxy-5'- phosphonylmethylpyrazofurin (13), 3'-fluoro-3'-deoxypyrazofurin (14), 1-deazapyrazofurin (15), 2-deazapyrazofurin (16), 2'-deoxypyrazofurin (17), and 3'-deoxypyrazofurin (18). Preparation of 5'-nor hydroxymethyl pyrazofurin (19) has been completed and this derivative will be submitted shortly for antiviral analysis. Only 2 and 6 showed any activity (versus vaccinia virus for 2 and influenza B for 6), which was not an improvement relative to pyrazofurin None of the compounds displayed meaningful cytotoxicity.
Document Details
- Document Type
- Technical Report
- Publication Date
- Jul 18, 1992
- Accession Number
- ADB168005
Entities
People
- Stewart W. Schneller
Organizations
- University of South Florida