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New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors.

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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

Edité par CCSD ; American Chemical Society -

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 highly active against the multidrug resistant mutant IRLL98 HIV-1 strain bearing the K101Q, Y181C, and G190A mutations conferring resistance to NVP, DLV, and EFV and several HIV-1 clades A in PBMC.

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