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

…, K Campanale, BA Heinz, LA Shipley…

Index: Victor, Frantz; Brown, Thomas J.; Campanale, Kristina; Heinz, Beverly A.; Shipley, Lisa A.; Su, Kenneth S.; Tang, Joseph; Vance, Lori M.; Spitzer, Wayne A. Journal of Medicinal Chemistry, 1997 , vol. 40, # 10 p. 1511 - 1518

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Citation Number: 48

Abstract

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 ...