title: Evaluation of a series of anticonvulsant 1,2,3,4-tetrahydroisoquinolinyl-benzamides.
abstract: SAR studies around a series of N-(tetrahydroisoquinolinyl)-2-methoxybenzamides, identified by high-throughput screening at the novel SB-204269 binding site, have provided compounds such as 13, 29-33 with high affinity and excellent anticonvulsant activity in animal models.
authors.affiliation: SmithKline Beecham Pharmaceuticals, Harlow, Essex, UK.
authors.forename: W N
authors.initials: WN
authors.lastname: Chan
authors.forename: M S
authors.initials: MS
authors.lastname: Hadley
authors.forename: J D
authors.initials: JD
authors.lastname: Harling
authors.forename: H J
authors.initials: HJ
authors.lastname: Herdon
authors.forename: B S
authors.initials: BS
authors.lastname: Orlek
authors.forename: G J
authors.initials: GJ
authors.lastname: Riley
authors.forename: R E
authors.initials: RE
authors.lastname: Stead
authors.forename: T O
authors.initials: TO
authors.lastname: Stean
authors.forename: M
authors.initials: M
authors.lastname: Thompson
authors.forename: N
authors.initials: N
authors.lastname: Upton
authors.forename: R W
authors.initials: RW
authors.lastname: Ward
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D001549:Benzamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D001578:Benzopyrans / Q000378:metabolism; D001665:Binding Sites; D001923:Brain Chemistry; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D007546:Isoquinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism / Q000494:pharmacology*; D008297:Male; D051379:Mice; D008958:Models, Molecular; D015394:Molecular Structure; D011869:Radioligand Assay; D051381:Rats; D012640:Seizures / Q000188:drug therapy; D013329:Structure-Activity Relationship
chemical_list: D000927:Anticonvulsants; D001549:Benzamides; D001578:Benzopyrans; D007546:Isoquinolines; C102319:SB 204269