Title of article :
New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central α2-antagonistic activity as potential antidepressants
Author/Authors :
Ludo E. J. Kennis، نويسنده , , François P. Bischoff، نويسنده , , Carolus J. Mertens، نويسنده , , Christopher J. Love، نويسنده , , Frans A. F. Van den Keybus، نويسنده , , Serge Pieters، نويسنده , , Mirielle Braeken، نويسنده , , Anton A. H. P. Megens، نويسنده , , Josee E. Leysen، نويسنده ,
Abstract :
The synthesis and biological activity of a series of benzofuro[3,2-c]pyridines and a benzothieno[3,2-c]pyridine are described. These compounds exhibit high affinity for the α2-adrenoceptor, with high selectivity versus the α1-receptor. Compound 1 also shows potent in vivo central activity and has been selected for further biological and clinical evaluation.