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N,N′-Linked 1,2-benzisothiazol-3(2H)-one 1,1-dioxides: synthesis, biological activity, and derived radicals |
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| Authors: | Valeria M Zakharova Ortwin Brede Mikhail A Kuznetsov Joachim Sieler |
| Institution: | a Faculty of Chemistry and Mineralogy, University of Leipzig, Johannisallee 29, Leipzig D-04103, Germany b St-Petersburg State University, Department of Organic Chemistry, University pr. 26, Saint-Petersburg 198504, Russia c Interdisciplinary Group of Time-Resolved Spectroscopy, University of Leipzig, Permoserstrasse 15, Leipzig D-04303, Germany d Pharmazeutisches Institut, Pharmazeutische Chemie I, Universität Bonn, An der Immenburg 4, Bonn D-53121, Germany |
| Abstract: | A number of N,N′-linked benzoannelated isothiazol-3(2H)-one 1,1-dioxides, not available via oxidation of isothiazolium salts, were obtained with good yields by reaction of N-amino heterocycles with 2-chlorosulfonylbenzoyl chloride and evaluated for their inhibitory activity toward human leukocyte elastase (HLE) and acetylcholinesterase (AChE). 2-(Phthalimid-1-yl)-1,2-benzisothiazol-3(2H)-one 1,1-dioxide and 2-(2-methyl-4-oxo-3(4H)-quinazolinyl)-1,2-benzisothiazol-3(2H)-one 1,1-dioxide were found to be inhibitors of HLE and tested as potential precursors of nitrogen-centered radicals using 266 nm laser flash photolysis. |
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