Title of article
Synthesis and biological evaluation of 3-aryltyramines as fragments binding to BACE-1 and BACE-2
Author/Authors
Fehler، نويسنده , , Stefanie K. and Pratsch، نويسنده , , Gerald and Huber، نويسنده , , Walter and Gast، نويسنده , , Alain and Hochstrasser، نويسنده , , Remo and Hennig، نويسنده , , Michael C Heinrich، نويسنده , , Markus R.، نويسنده ,
Issue Information
هفته نامه با شماره پیاپی سال 2012
Pages
6
From page
2189
To page
2194
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.
Keywords
radical reactions , BACE , Tyramine , Biaryl , arylation
Journal title
Tetrahedron Letters
Serial Year
2012
Journal title
Tetrahedron Letters
Record number
1880594
Link To Document