New Nitrogen Containing Substituents at the Indole-2-carboxamide Yield High Potent and Broad Spectrum Indolylarylsulfone HIV-1 Non-Nucleoside Reverse Transcriptase Inhibitors.


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 multi-drug 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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