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New 2-substituted 1,2,3,4-tetrahydrobenzofuro[3,2-c]pyridine having highly active and potent central alpha
L E Kennis1, F P Bischoff, C J Mertens
1Department of Medicinal Chemistry, Janssen Research Foundation, Beerse, Belgium. lkennis@janbe.jnj.com
Bioorganic & Medicinal Chemistry Letters
|January 15, 2000
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 alpha 2-adrenoceptor, with high selectivity versus the alpha 1-receptor. Compound 1 also shows potent in vivo central activity and has been selected for further biological and clinical evaluation.