Identification of a novel series of selective 5-HT7 receptor antagonists

Ian T Forbes; David G Cooper; Emma K Dodds; Sara E Douglas; Andrew D Gribble; Robert J Ife; Andrew P Lightfoot; Malcolm Meeson; Lorraine P Campbell; Tanya Coleman; Graham J Riley; David R Thomas

doi:10.1016/s0960-894x(03)00077-5

Identification of a novel series of selective 5-HT7 receptor antagonists

Bioorg Med Chem Lett. 2003 Mar 24;13(6):1055-8. doi: 10.1016/s0960-894x(03)00077-5.

Authors

Ian T Forbes¹, David G Cooper, Emma K Dodds, Sara E Douglas, Andrew D Gribble, Robert J Ife, Andrew P Lightfoot, Malcolm Meeson, Lorraine P Campbell, Tanya Coleman, Graham J Riley, David R Thomas

Affiliation

¹ GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK.

PMID: 12643910
DOI: 10.1016/s0960-894x(03)00077-5

Abstract

Novel 5-HT(7) receptor antagonists containing the benzocycloheptanone core were identified from high throughput screening. Molecular modelling and SAR studies have converted these intractable hits into a more potent, selective and tractable series, exemplified by compound (25), SB-691673.

MeSH terms

Cytochrome P-450 Enzyme System / drug effects
Drug Design
Drug Evaluation, Preclinical
Humans
Indicators and Reagents
Isoenzymes / drug effects
Models, Molecular
Receptors, Serotonin / drug effects*
Serotonin Antagonists / chemical synthesis*
Serotonin Antagonists / pharmacology*
Structure-Activity Relationship

Substances

Indicators and Reagents
Isoenzymes
Receptors, Serotonin
Serotonin Antagonists
serotonin 7 receptor
Cytochrome P-450 Enzyme System