Novel benzofuran derivatives with dual 5-HT1A receptor and serotonin transporter affinity

Aranapakam M Venkatesan; O Dos Santos; John Ellingboe; Deborah A Evrard; Boyd L Harrison; Deborah L Smith; Rosemary Scerni; Geoffrey A Hornby; Lee E Schechter; Terrence H Andree

doi:10.1016/j.bmcl.2009.12.093

Novel benzofuran derivatives with dual 5-HT1A receptor and serotonin transporter affinity

Bioorg Med Chem Lett. 2010 Feb 1;20(3):824-7. doi: 10.1016/j.bmcl.2009.12.093. Epub 2010 Jan 4.

Authors

Aranapakam M Venkatesan¹, O Dos Santos, John Ellingboe, Deborah A Evrard, Boyd L Harrison, Deborah L Smith, Rosemary Scerni, Geoffrey A Hornby, Lee E Schechter, Terrence H Andree

Affiliation

¹ Chemical Sciences, Wyeth Research, Pearl River, NY 10965, United States.

PMID: 20064720
DOI: 10.1016/j.bmcl.2009.12.093

Abstract

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.

Publication types

Comparative Study

MeSH terms

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

Substances

Benzofurans
Serotonin Plasma Membrane Transport Proteins
Receptor, Serotonin, 5-HT1A
benzofuran