title: Synthesis of some new benzisothiazolone and benzenesulfonamide derivatives of biological interest starting from saccharin sodium.
abstract: 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.
authors.affiliation: Faculty of Pharmacy, Pharmaceutical Chemistry Department, Taif University, Taif, Saudi Arabia; Faculty of Pharmacy, Medicinal Chemistry Department, Zagazig University, Zagazig, Egypt.
authors.forename: Osama I
authors.initials: OI
authors.lastname: El-Sabbagh
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D002478:Cells, Cultured; D006801:Humans; D008168:Lung / Q000166:cytology; D051379:Mice; D012439:Saccharin / Q000737:chemistry; D013057:Spectrum Analysis; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013844:Thiazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D014780:Viruses / Q000187:drug effects*; D000096926:Benzenesulfonamides
chemical_list: D000998:Antiviral Agents; D012439:Saccharin; D013449:Sulfonamides; D013844:Thiazoles; D000096926:Benzenesulfonamides; C015699:1,2-benzisothiazoline-3-one
keywords: Antiviral activity; Benzenesulfonamide; Benzisothiazolone derivatives; Saccharin sodium; Synthesis