Chan W N, Hadley M S, Harling J D, Herdon H J, Orlek B S, Riley G J, Stead R E, Stean T O, Thompson M, Upton N, Ward R W
SmithKline Beecham Pharmaceuticals, Harlow, Essex, UK.
Bioorg Med Chem. 2000 Aug;8(8):2085-94. doi: 10.1016/s0968-0896(00)00149-8.
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.
围绕一系列在新型SB-204269结合位点通过高通量筛选鉴定出的N-(四氢异喹啉基)-2-甲氧基苯甲酰胺进行的构效关系研究,已得到在动物模型中具有高亲和力和优异抗惊厥活性的化合物,如13、29 - 33。