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.
Scheda prodotto non validato
Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo
Titolo: | Anti-HIV evaluation of benzo[d]isothiazole hydrazones |
Autori: | |
Data di pubblicazione: | 2009 |
Rivista: | |
Abstract: | 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. |
Handle: | http://hdl.handle.net/11584/23149 |
Tipologia: | 1.1 Articolo in rivista |