Synthesis of some new benzisothiazolone and benzenesulfonamide derivatives of biological interest starting from saccharin sodium.

Two new series of benzenesulfonamide (4a-f, 5a-b, 6, 7) and 1,2-benzisothiazol-3(2H)-one-1,1-dioxide (9a-c, 10, 12a-d) derivatives were prepared starting from saccharin sodium. The novel compounds were characterized using elemental analyses and different spectroscopic methods. Assessment of the antiviral activities of these novel compounds against a broad panel of viruses in different cell cultures revealed that only the thiazole derivatives belonging to the benzisothiazol-3(2H)-one-1,1-dioxide series are the active ones. All thiazole derivatives 12a-d showed activity against both varicella-zoster virus, especially TK(-) VZV strain 07-1, and the cytomegalovirus strains AD-169 and Davis in human embryonic lung (HEL) cell culture.