Article
Thiotetrazole alkynylacetanilides as potent and bioavailable non-nucleoside inhibitors of the HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases.
Bioorganic & medicinal chemistry letters - 15 Aug 2007
Gagnon Alexandre, Amad Ma'an H, Bonneau Pierre R, Coulombe René, DeRoy Patrick L, Doyon Louise, Duan Jianmin, Garneau Michel, Guse Ingrid, Jakalian Araz, Jolicoeur Eric, Landry Serge, Malenfant Eric, Simoneau Bruno, Yoakim Christiane
Abstract excerpt
A series of aryl thiotetrazolylacetanilides were synthesized and found to be potent inhibitors of the HIV-1 wild type and K103N/Y181C double mutant reverse transcriptases. The incorporation of an alkynyl fragment on the aniline provided inhibitors with excellent cellular activity and extensive SAR led to the identification of one inhibitor having good oral bioavailability in rats.
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