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

Giuseppe La Regina, Antonio Coluccia, Andrea Brancale, Francesco Piscitelli, Valeria Famiglini, Sandro Cosconati, Giovanni Maga, Alberta Samuele, Emmanuel Gonzalez, Bonaventura Clotet, Dominique Schols, José A. Esté, Ettore Novellino, Romano Silvestri

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44 Citations (Scopus)

Abstract

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. © 2012 American Chemical Society.
Original languageEnglish
Pages (from-to)6634-6638
JournalJournal of Medicinal Chemistry
Volume55
Issue number14
DOIs
Publication statusPublished - 26 Jul 2012

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