New 2-substituted 1, 2, 3, 4-tetrahydrobenzofuro [3, 2-c] pyridine having highly active and potent central α 2-antagonistic activity as potential antidepressants

…, FAF Van den Keybus, S Pieters, M Braeken…

Index: Kennis, Ludo E.J.; Bischoff, Francois P.; Mertens, Carolus J.; Love, Christopher J.; Van den Keybus, Frans A.F.; Pieters, Serge; Braeken, Mirielle; Megens, Anton A.H.P.; Leysen, Josee E. Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 1 p. 71 - 74

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Citation Number: 39

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.