Synthesis of Some New Benzisothiazolone and Benzenesulfonamide Derivatives of Biological Interest Starting from Saccharin Sodium

Faculty Pharmacy Year: 2013
Type of Publication: Article Pages: 733-742
Authors: DOI: 10.1002/ardp.201300110
Journal: ARCHIV DER PHARMAZIE WILEY-V C H VERLAG GMBH Volume: 346
Research Area: Pharmacology \& Pharmacy; Chemistry ISSN ISI:000325497500005
Keywords : Antiviral activity, Benzenesulfonamide, Benzisothiazolone derivatives, Saccharin sodium, Synthesis    
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.
   
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