The p-fluoro derivative 12 of Enviroxime vinylacetylene analogs demonstrates oral bioavailability and in vivo efficacy against Coxsackie A21 infection in mice.
Advances oral antiviral candidates for enteroviral disease; leaves open clinical validation in humans.
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.
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Victor et al. (1997) studied this question.
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