Article
Tetrazole thioacetanilides: potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant.
Bioorganic & medicinal chemistry letters - 15 May 2006
Muraglia Ester, Kinzel Olaf D, Laufer Ralph, Miller Michael D, Moyer Gregory, Munshi Vandna, Orvieto Federica, Palumbi Maria Cecilia, Pescatore Giovanna, Rowley Michael, Williams Peter D, Summa Vincenzo
Abstract excerpt
A series of aryltetrazolylacetanilides was synthesized and evaluated as HIV-1 non-nucleoside reverse transcriptase inhibitors on wild-type virus and on the clinically relevant K103N mutant strain. Extensive SAR investigation led to potent compounds, with nanomolar activity on K103N, and orally bioavailable in rats.
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