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  • Title: Anti-HIV evaluation of benzo[d]isothiazole hydrazones.
    Author: Vicini P, Incerti M, La Colla P, Loddo R.
    Journal: Eur J Med Chem; 2009 Apr; 44(4):1801-7. PubMed ID: 18614259.
    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 (EFV(R), Y181C and K103/Y181C) showed good activity against wild type HIV-1 and against the EFV(R) 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.
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