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Beschreibungen/Notizen
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.
High-throughput screening with the selective ligand [
3H] SB-204269 has revealed a series of tetrahydroisquinolinyl benzamides
2–18. Preliminary SAR analysis has led to the 5-isomer
4 (R=2-OMe, 4-Bu
t) which showed high affinity and a good anticonvulsant profile
in vivo.