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Synthesis and biological evaluation of 3-aryltyramines as fragments binding to BACE-1 and BACE-2 |
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| Authors: | Stefanie K Fehler Gerald Pratsch Walter Huber Alain Gast Remo Hochstrasser Michael Hennig Markus R Heinrich |
| Institution: | 1. Department für Chemie und Pharmazie, Pharmazeutische Chemie, Friedrich-Alexander-Universität Erlangen-Nürnberg, Schuhstraße 19, 91052 Erlangen, Germany;2. F. Hoffmann-La Roche Ltd., Discovery Technologies, 4070 Basel 65/319, Switzerland |
| Abstract: | 3-Aryltyramines were prepared in one single step from tyramine and various arenediazonium salts by radical arylation. Binding as well as enzyme inhibition data of the 14 compounds do not prove true interaction with BACE-1. In contrast, with BACE-2 inhibition and binding could be confirmed indicating that 3-aryltyramines are potential starting points for a drug discovery effort. |
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