Chemistry of Biologically Active Isothiazoles

Complete 1H and 13C NMR spectral assignment of benzo[d]isothiazole derivatives and of an isoindole isoster

“…For a number of years, we have designed, synthetized and tested series of 3-substituted benzisothiazole derivatives [3 -10] and more recently, we have discovered novel 2-aminobenzo[d]isothiazole-3-one derivatives displaying new, interesting biological properties. [11 -14] Although a lot of structural data have been reported in the literature concerning the chemistry of the benzofused isothiazoles, [1,2,15] detailed information about 1 H and 13 C NMR signals of the class of compounds is still lacking. In pursuing studies on this class of benzisothiazole derivatives, structural elucidation is a significant part of our work.…”

“…[1,2] The benzo [d]isothiazole ring can be a substituent of a bioactive scaffold or the pharmacophore of a bioactive molecule. For a number of years, we have designed, synthetized and tested series of 3-substituted benzisothiazole derivatives [3 -10] and more recently, we have discovered novel 2-aminobenzo[d]isothiazole-3-one derivatives displaying new, interesting biological properties.…”

Anti-HIV evaluation of benzo[d]isothiazole hydrazones

“…Interestingly, compounds sharing a benzisothiazole skeleton have shown biological activity [8,9]. Namely, derivatives endowed with antimicrobial [10], antipsychotic [11] and anti-human leukocyte elastase [12] activities have been reported.…”

Hybrid molecules between benzenesulfonamides and active antimicrobial benzo[d]isothiazol-3-ones

“…Benzo [d]isothiazol-3-ones are a class of heterocyclic compounds endowed with a broad spectrum of biological activity [1,2]. They have been reported to possess antiplatelet and spasmolytic effects [3,4] and they attracted a great deal of interest particularly on the antimicrobial activity.…”