Evaluation of a series of anticonvulsant 1,2,3,4-tetrahydroisoquinolinyl-benzamides.
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.
Chan
W N
WN
SmithKline Beecham Pharmaceuticals, Harlow, Essex, UK.
Hadley
M S
MS
Harling
J D
JD
Herdon
H J
HJ
Orlek
B S
BS
Riley
G J
GJ
Stead
R E
RE
Stean
T O
TO
Thompson
M
M
Upton
N
N
Ward
R W
RW
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
D000927:Anticonvulsants; D001549:Benzamides; D001578:Benzopyrans; D007546:Isoquinolines; C102319:SB 204269