2 research outputs found
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 <b>9</b> 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
2-(Alkyl/Aryl)Amino-6-Benzylpyrimidin-4(3<i>H</i>)-ones as Inhibitors of Wild-Type and Mutant HIV-1: Enantioselectivity Studies
The single enantiomers of two pyrimidine-based HIV-1
non-nucleoside
reverse transcriptase inhibitors, <b>1</b> (MC1501) and <b>2</b> (MC2082), were tested in both cellular and enzyme assays.
In general, the <i>R</i> forms were more potent than their <i>S</i> counterparts and racemates and (<i>R</i>)-<b>2</b> was more efficient than (<i>R</i>)-<b>1</b> and the reference compounds, with some exceptions. Interestingly,
(<i>R</i>)-<b>2</b> displayed a faster binding to
K103N RT with respect to WT RT, while (<i>R</i>)-<b>1</b> showed the opposite behavior