Anti-HIV evaluation of benzo[d]isothiazole hydrazones

The synthesis and the anti-HIV-1 activity of novel benzo[d]isothiazole hydrazones are reported. Target compounds tested in MT-4 cells cultures for their anti-HIV properties against wild type HIV-1 and HIV strains carrying clinically relevant mutations (EFVR, Y181C and K103/Y181C) showed good activity against wild type HIV-1 and against the EFVR mutant. In terms of SAR the relevant result was that, in the class of benzisothiazole hydrazones, the benzo[d]isothiazol-3(2H)-one moiety (compounds 1 and 4) is an essential structural requirement for the antiretroviral activity.

Graphical abstractThe synthesis and the anti-HIV-1 activity of novel benzo[d]isothiazole hydrazones are reported. The presence of the benzo[d]isothiazol-3(2H)-one moiety (compounds 1 and 4) is an essential structural requirement for the antiretroviral activity.Figure optionsDownload full-size imageDownload as PowerPoint slide