Article
New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.
Journal of medicinal chemistry - 26 Jul 2012
La Regina Giuseppe, Coluccia Antonio, Brancale Andrea, Piscitelli Francesco, Famiglini Valeria, Cosconati Sandro, Maga Giovanni, Samuele Alberta, Gonzalez Emmanuel, Clotet Bonaventura, Schols Dominique, Esté José A, Novellino Ettore, Silvestri Romano
Abstract excerpt
New indolylarylsulfone (IAS) derivatives bearing nitrogen containing substituents at the indole-2-carboxamide inhibited the HIV-1 WT in MT-4 cells at low nanomolar concentrations. In particular, compound 9 was uniformly effective against the mutant Y181C, Y188L, and K103N HIV-1 strains; it was hi...
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