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.
MeSH terms
-
Animals
-
Anticonvulsants / chemical synthesis
-
Anticonvulsants / chemistry*
-
Anticonvulsants / metabolism
-
Anticonvulsants / pharmacology*
-
Benzamides / chemical synthesis
-
Benzamides / chemistry*
-
Benzamides / metabolism
-
Benzamides / pharmacology*
-
Benzopyrans / metabolism
-
Binding Sites
-
Brain Chemistry
-
Drug Design*
-
Drug Evaluation, Preclinical
-
Isoquinolines / chemical synthesis
-
Isoquinolines / chemistry*
-
Isoquinolines / metabolism
-
Isoquinolines / pharmacology*
-
Male
-
Mice
-
Models, Molecular
-
Molecular Structure
-
Radioligand Assay
-
Rats
-
Seizures / drug therapy
-
Structure-Activity Relationship
Substances
-
Anticonvulsants
-
Benzamides
-
Benzopyrans
-
Isoquinolines
-
SB 204269