Published in
American Chemical Society, Journal of Medicinal Chemistry, 14(55), p. 6634-6638, 2012
DOI: 10.1021/jm300477h
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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
,
Andrea Brancale,
Francesco Piscitelli,
Valeria Famiglini,
Sandro Cosconati ,
Giovanni Maga,
Alberta Samuele,
E. Gonzales,
Emmanuel Gonzalez,
Bonaventura Clotet,
Dominique Schols,
José A. Esté,
Ettore Novellino,
Romano Silvestri
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- Must not violate ACS ethical Guidelines
- Must obtain written permission from Editor
- Must not violate ACS ethical Guidelines
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.