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 :
بازگشت