Identification of a series of 1,2,3,4-tetrahydroisoquinolinyl-benzamides with potential anticonvulsant activity.
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.
Chan
W N
WN
SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, Harlow, Essex, UK.
Hadley
M S
MS
Harling
J D
JD
Herdon
H J
HJ
Jerman
J C
JC
Orlek
B S
BS
Stean
T O
TO
Thompson
M
M
Upton
N
N
Ward
R W
RW
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
D000927:Anticonvulsants; D001549:Benzamides; D001578:Benzopyrans; D011804:Quinolines; C102319:SB 204269