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 (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.
Vicini
Paola
P
Dipartimento Farmaceutico, Università degli Studi di Parma, Via G.P. Usberti 27/A, Parma 43100, Italy. paola.vicini@unipr.it
Incerti
Matteo
M
La Colla
Paolo
P
Loddo
Roberta
R
D019380:Anti-HIV Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D006678:HIV / Q000187:drug effects*; D006801:Humans; D006835:Hydrazones / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity
D019380:Anti-HIV Agents; D006835:Hydrazones