Article
4-benzyl- and 4-benzoyl-3-dimethylaminopyridin-2(1H)-ones, a new family of potent anti-HIV agents: optimization and in vitro evaluation against clinically important HIV mutant strains.
Journal of medicinal chemistry - 21 Oct 2004
Benjahad Abdellah, Courté Karine, Guillemont Jérôme, Mabire Dominique, Coupa Sophie, Poncelet Alain, Csoka Imre, Andries Koen, Pauwels Rudi, de Béthune Marie-Pierre, Monneret Claude, Bisagni Emile, Nguyen Chi Hung, Grierson David S
Abstract excerpt
The 4-benzyl and 4-benzoyl-3-dimethylaminopyridinones 13 and 14 are representatives of a new class of highly potent non nucleoside type inhibitors of HIV-1 reverse transcriptase. To conduct SAR studies on these two lead compounds, 102 new analogues were prepared. Thirty-three compounds displayed nanomolar range activity in vitro against wild-type HIV-1, and among these, 18 were active against the 103N, Y181C, and...
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