Novel benzofuran derivatives with dual 5-HT1A receptor and serotonin transporter affinity.
Several benzofuran derivatives linked to a 3-indoletetrahydropyridine through an alkyl chain were prepared and evaluated for serotonin transporter and 5-HT(1A) receptor affinities. Their design, synthesis and structure-activity relationships are described.
Venkatesan
Aranapakam M
AM
Chemical Sciences, Wyeth Research, Pearl River, NY 10965, United States.
Dos Santos
O
O
Ellingboe
John
J
Evrard
Deborah A
DA
Harrison
Boyd L
BL
Smith
Deborah L
DL
Scerni
Rosemary
R
Hornby
Geoffrey A
GA
Schechter
Lee E
LE
Andree
Terrence H
TH
D000818:Animals; D001572:Benzofurans / Q000737:chemistry* / Q000378:metabolism*; D016466:CHO Cells; D006224:Cricetinae; D003412:Cricetulus; D006801:Humans; D011485:Protein Binding / Q000502:physiology; D044282:Receptor, Serotonin, 5-HT1A / Q000378:metabolism*; D050486:Serotonin Plasma Membrane Transport Proteins / Q000378:metabolism*; D013329:Structure-Activity Relationship
D001572:Benzofurans; D050486:Serotonin Plasma Membrane Transport Proteins; D044282:Receptor, Serotonin, 5-HT1A; C105430:benzofuran