189061-08-3Relevant articles and documents
Synthesis, antiviral activity, and biological properties of vinylacetylene analogs of enviroxime
Victor, Frantz,Brown, Thomas J.,Campanale, Kristina,Heinz, Beverly A.,Shipley, Lisa A.,Su, Kenneth S.,Tang, Joseph,Vance, Lori M.,Spitzer, Wayne A.
, p. 1511 - 1518 (2007/10/03)
A series of vinylacetylene analogs of Enviroxime (1) was synthesized. The new compounds are potent inhibitors of poliovirus in tissue culture. Cross-sensitivity with Enviroxime-derived mutants shows that the new compounds have the same mechanism of action as Enviroxime, which involves the viral 3A protein. In studies with Rhesus monkeys, the p-fluoro derivative 12 was found to be unique in providing oral bioavailability. Metabolism studies using hepatic microsomes suggest that this procedure would be a useful in vitro method for selecting the appropriate animal model for testing oral absorption. Compound 12 was found to be efficacious by oral administration in treating a Coxsackie A21 infection in CD-1 mice.