一系列具有潜在抗惊厥活性的1,2,3,4-四氢异喹啉基-苯甲酰胺的鉴定。
Identification of a series of 1,2,3,4-tetrahydroisoquinolinyl-benzamides with potential anticonvulsant activity.
作者信息
Chan W N, Hadley M S, Harling J D, Herdon H J, Jerman J C, Orlek B S, Stean T O, Thompson M, Upton N, Ward R W
机构信息
SmithKline Beecham Pharmaceuticals, New Frontiers Science Park, Harlow, Essex, UK.
出版信息
Bioorg Med Chem Lett. 1998 Oct 20;8(20):2903-6. doi: 10.1016/s0960-894x(98)00523-x.
PMID:9873645
Abstract
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.
摘要
通过在新型SB - 204269结合位点进行高通量筛选，鉴定出一系列N -（四氢异喹啉基）- 2 - 甲氧基苯甲酰胺。构效关系研究已在动物模型中提供了具有高亲和力和良好抗惊厥活性的化合物4和14。
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