Walker K A, Wallach M B, Hirschfeld D R
J Med Chem. 1981 Jan;24(1):67-74. doi: 10.1021/jm00133a015.
Potent anticonvulsant activity has been demonstrated for a large number of 1-(naphthylalkyl)-1H-imidazoles containing a variety of functional groups in the alkylene bridge. The presence of a small oxygen function in the bridge, in general, confers a high therapeutic index between anticonvulsant and depressant activity. Clinical expectations are discussed for 1-(2-naphthoylmethyl)imidazole hydrochloride (5), which is undergoing development for testing in humans.
大量在亚烷基桥中含有各种官能团的1-(萘基烷基)-1H-咪唑已显示出强大的抗惊厥活性。通常,桥中存在一个小的氧官能团会在抗惊厥活性和抑制活性之间赋予较高的治疗指数。文中讨论了1-(2-萘甲酰甲基)咪唑盐酸盐(5)的临床应用前景,该药物正在进行人体试验开发。