化学
抗惊厥药
苯甲酰胺
芳基
酰胺
立体化学
羟甲基
戒指(化学)
化学合成
有机化学
癫痫
生物化学
体外
生物
神经科学
烷基
作者
F. Lepage,F. Tombret,G. Cuvier,A. MARIVAIN,J. M. Gillardin
标识
DOI:10.1016/0223-5234(92)90137-p
摘要
We prepared a series of N-aryl isoxazolecarboxamide, N-isoxazolylbenzamide compounds and derivatives and studied their anticonvulsant action in MES and MMS tests. Some of these reveal considerable activity, especially with respect to MES test. The disubstitution in the 2.6-position on the phenyl ring by two methyl groups would appear to be of primary importance for the activity. The amide bridge between the phenyl and isoxazolic rings, whether of the anilide or benzamide type, seems to show similar anticonvulsant behavior. We have selected the derivatives 8 (N-(2.6-dimethylphenyl)-5-methyl-3-isoxazolecarboxamide, 12 (N-(2.6-dimethylphenyl)-5-hydroxymethyl-3-isoxazolecarboxamide) and 51 (N-(5-methyl-3-isoxazolyl)-2.6-dimethylbenzamide) which are presently being studied in more extended pharmacological tests.
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