title: Identification of a series of 1,2,3,4-tetrahydroisoquinolinyl-benzamides with potential anticonvulsant activity.
abstract: A series of N-(tetrahydroisoquinolinyl)-2-methoxybenzamides was identified by high-throughput screening at the novel SB-204269 binding site. SAR studies have provided compounds 4 and 14 with high affinity and good anticonvulsant activity in animal models.
authors.affiliation: SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, 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: J C
authors.initials: JC
authors.lastname: Jerman
authors.forename: B S
authors.initials: BS
authors.lastname: Orlek
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 / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D001549:Benzamides / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D001578:Benzopyrans / Q000494:pharmacology; D001665:Binding Sites; D051379:Mice; D008958:Models, Molecular; D011804:Quinolines / Q000737:chemistry* / Q000494:pharmacology / Q000627:therapeutic use; D012640:Seizures / Q000517:prevention & control; D013329:Structure-Activity Relationship
chemical_list: D000927:Anticonvulsants; D001549:Benzamides; D001578:Benzopyrans; D011804:Quinolines; C102319:SB 204269