Identification of a novel series of selective 5-HT7 receptor antagonists.
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.
Forbes
Ian T
IT
GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK.
Cooper
David G
DG
Dodds
Emma K
EK
Douglas
Sara E
SE
Gribble
Andrew D
AD
Ife
Robert J
RJ
Lightfoot
Andrew P
AP
Meeson
Malcolm
M
Campbell
Lorraine P
LP
Coleman
Tanya
T
Riley
Graham J
GJ
Thomas
David R
DR
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
D007202:Indicators and Reagents; D007527:Isoenzymes; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; C104425:serotonin 7 receptor; D003577:Cytochrome P-450 Enzyme System