title: Identification of a novel series of selective 5-HT7 receptor antagonists.
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.
authors.affiliation: GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK.
authors.forename: Ian T
authors.initials: IT
authors.lastname: Forbes
authors.forename: David G
authors.initials: DG
authors.lastname: Cooper
authors.forename: Emma K
authors.initials: EK
authors.lastname: Dodds
authors.forename: Sara E
authors.initials: SE
authors.lastname: Douglas
authors.forename: Andrew D
authors.initials: AD
authors.lastname: Gribble
authors.forename: Robert J
authors.initials: RJ
authors.lastname: Ife
authors.forename: Andrew P
authors.initials: AP
authors.lastname: Lightfoot
authors.forename: Malcolm
authors.initials: M
authors.lastname: Meeson
authors.forename: Lorraine P
authors.initials: LP
authors.lastname: Campbell
authors.forename: Tanya
authors.initials: T
authors.lastname: Coleman
authors.forename: Graham J
authors.initials: GJ
authors.lastname: Riley
authors.forename: David R
authors.initials: DR
authors.lastname: Thomas
mesh_terms: D003577:Cytochrome P-450 Enzyme System / Q000187:drug effects; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007202:Indicators and Reagents; D007527:Isoenzymes / Q000187:drug effects; D008958:Models, Molecular; D011985:Receptors, Serotonin / Q000187:drug effects*; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D007202:Indicators and Reagents; D007527:Isoenzymes; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; C104425:serotonin 7 receptor; D003577:Cytochrome P-450 Enzyme System