抗惊厥药。5. 5-乙基-5-苯基乙内酰脲和5,5-二苯基乙内酰脲的衍生物。
Anticonvulsants. 5. Derivatives of 5-ethyl-5-phenylhydantoin and 5,5-diphenylhydantoin.
作者信息
Vida J A, O'Dea M H, Samour C M, Reinhard J F
出版信息
J Med Chem. 1975 Apr;18(4):383-5. doi: 10.1021/jm00238a012.
Alkoxymethyl, acyloxymethyl, and mixed alkylalkoxymethyl or alkylacyloxymethyl derivatives of 5-ethyl-5-phenylhydantoin exhibit anticonvulsant activity. Also effective are bis(alkoxymethyl) and mixed alkylalkoxymethyl derivatives of 5,5-diphenylhydantoin. Of particular interest are 1,3-bis(methoxymethyl)-5,5-diphenylhydantoin and 3-acetoxymethyl-5-ethyl-5-phenylhydantoin, which show good activity against maximal electroshock seizures, and 3-methoxymethyl-5-ethyl-5-phenylhydantoin, which is effective against both maximal electroshock and pentylenetetrazole. None of the above compounds show greater activity against maximal electroshock seizures than the parent compounds, however.
5-乙基-5-苯基乙内酰脲的烷氧甲基、酰氧甲基以及混合的烷基烷氧甲基或烷基酰氧甲基衍生物具有抗惊厥活性。5,5-二苯基乙内酰脲的双（烷氧甲基）和混合的烷基烷氧甲基衍生物也有效。特别值得关注的是1,3-双（甲氧基甲基）-5,5-二苯基乙内酰脲和3-乙酰氧甲基-5-乙基-5-苯基乙内酰脲，它们对最大电休克惊厥显示出良好活性，以及3-甲氧基甲基-5-乙基-5-苯基乙内酰脲，其对最大电休克和戊四氮均有效。然而，上述化合物对最大电休克惊厥的活性均不高于母体化合物。
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