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.
Anti-HIV evaluation of benzo[d]isothiazole hydrazones / Vicini, Paola; Incerti, Matteo; LA COLLA, P.; Loddo, R.. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - 44:(2009), pp. 1801-1807. [10.1016/J.EJMECH.2008.05.030]
Anti-HIV evaluation of benzo[d]isothiazole hydrazones.
VICINI, Paola;INCERTI, Matteo;
2009-01-01
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.| File | Dimensione | Formato | |
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