Accession Number : ADB168005

Title :   Synthesis and Antiviral Evaluation of Pyrazofurin Analogues.

Descriptive Note : Final rept. 19 Jun 89-18 Jun 92,

Corporate Author : UNIVERSITY OF SOUTH FLORIDA TAMPA

Personal Author(s) : Schneller, Stewart W.

Report Date : 18 JUL 1992

Pagination or Media Count : 149

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.

Descriptors :   *ANTIVIRAL AGENTS, *PYRAZOLES, *SYNTHESIS, AMIDES, ARMY, DISTRIBUTION, INFLUENZA, MARYLAND, MEDICAL RESEARCH, PREPARATION, PYRROLES, CELLS(BIOLOGY), TEST AND EVALUATION, IN VITRO ANALYSIS, CULTURES(BIOLOGY), TOXICITY, .

Subject Categories : Pharmacology
      Organic Chemistry

Distribution Statement : APPROVED FOR PUBLIC RELEASE