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Synthesis of 4‐(Isothiazol‐3‐yl)morpholines and 1‐(Isothiazol‐3‐yl)piperazines,and Their Inhibitory Activity towards Acetylcholinesterase |
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| Authors: | Janine Wolf Camino?M?González Tanarro Michael Gütschow Joachim Sieler Bärbel Schulze |
| Institution: | 1. Institute of Organic Chemistry, University of Leipzig, Johannisallee 29, D‐04103, Leipzig, (fax: +49‐341‐9736599);2. Pharmaceutical Institute, University of Bonn, An der Immenburg 4, D‐53121 Bonn;3. Institute of Inorganic Chemistry, University of Leipzig, Johannisallee 29, D‐04103 Leipzig |
| Abstract: | The synthesis of novel triaryl‐substituted 4‐(isothiazol‐3‐yl)morpholines 7 and 8 , and 1‐(isothiazol‐3‐yl)piperazines 9 – 13 by reaction of the corresponding isothiazolium salts 5 and 6 with secondary amines in the presence of t‐BuOK in absolute THF is described. Some representatives of the isothiazoles were evaluated as inhibitors of acetylcholinesterase from Electrophorus electricus. |
| Keywords: | Acetylcholinesterase Inhibitors Isothiazolium salts Piperazines isothiazolyl‐ Morpholines isothiazolyl‐ |