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

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

  • J Med Chem. 2012 Jul 26;55(14):6634-8. doi: 10.1021/jm300477h.
Giuseppe La Regina 1,  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
Affiliations

Affiliation

  • 1 Istituto Pasteur - Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Piazzale Aldo Moro 5, I-00185 Roma, Italy.
PMID: 22712652 DOI: 10.1021/jm300477h
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.

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