Synthesis, antiviral activity, and biological properties of vinylacetylene analogs of enviroxime
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.
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)
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