Anti-HIV evaluation of benzo[d]isothiazole hydrazones

作者：Vicini Paola^*; Incerti Matteo; La Colla Paolo; Loddo Roberta

来源：European Journal of Medicinal Chemistry, 2009, 44(4): 1801-1807.

DOI：10.1016/j.ejmech.2008.05.030

• Benzo[d]isothiazole hydrazones
• Benzo[d]isothiazol-3-one derivatives
• Antiviral activity
• Anti-HIV-1 activity

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 (EFV(R), 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 anti-retroviral activity.

• 出版日期2009-4