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.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-02, Vol.20 (3), p.824-827
Hauptverfasser:	Venkatesan, Aranapakam M, Dos Santos, O, Ellingboe, John, Evrard, Deborah A, Harrison, Boyd L, Smith, Deborah L, Scerni, Rosemary, Hornby, Geoffrey A, Schechter, Lee E, Andree, Terrence H
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Benzofurans - chemistry Benzofurans - metabolism CHO Cells Cricetinae Cricetulus Humans Protein Binding - physiology Receptor, Serotonin, 5-HT1A - metabolism Serotonin Plasma Membrane Transport Proteins - metabolism Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2009.12.093