Matteo Incerti

TL;DR: The results highlighted that all the benzo[d]isothiazole derivatives inhibited the growth of leukaemia cell lines, whereas only one of the above mentioned compounds showed antiproliferative activity against two solid tumor-derived cell lines.

TL;DR: The 5-arylidene derivatives showed an antibacterial efficacy considerably greater than that of the parent 2-(thiazol-2-ylimino)thiazolidin-4-one 3, suggesting that the substituted and unsubstituted 5- Darylidene moiety plays an important role in enhancing the antimicrobial properties of this class of compounds.

TL;DR: 2h proved to be the most active compound and the fragment -CO-NH-N=CH-2-hydroxyphenyl was identified as being very important for biological activity, suggesting intramolecular hydrogen bond formation or favourable mutual disposition between two important centres in the pharmacophore.

TL;DR: It is worth noting that the replacement of the thiazole nucleus for the benzo[d]thiazole bicyclic system in the parent 2-(benzylidene-2-ylimino)thiazolidin-4-one leads to significant antifungal properties against both yeasts and moulds, properties not shown by the analogous 2-thiazolyl- and 2-benzo[ d]isothiazoly l-imino-5-

TL;DR: The synthesis and the anti-HIV-1 activity of novel benzo[d]isothiazol-3(2H)-one moiety is reported and the essential structural requirement for the antiretroviral activity is found.