New nitrogen containing substituents at the indole-2-carboxamide yield high potent and broad spectrum indolylarylsulfone HIV-1 non-nucleoside reverse transcriptase inhibitors
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 #
Journal of Medicinal Chemistry vol:55 issue:14 pages:6634-6638
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.