6-(ALKYLAMINO)-9-BENZYL-9H-PURINES - A NEW CLASS OF ANTICONVULSANT AGENTS
6-(ALKYLAMINO)-9-BENZYL-9H-PURINES - A NEW CLASS OF ANTICONVULSANT AGENTS
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DOI：
10.1021/jm00398a019
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发表时间：
1988-03-01
影响因子：
7.3
通讯作者：
SOROKO, FE
中科院分区：
文献类型：
--
作者：
KELLEY, JL;KROCHMAL, MP;SOROKO, FE
合成了几种9-烷基-6-取代嘌呤类化合物，并测定了它们对大鼠最大电休克诱发癫痫发作（MES）的抗惊厥活性。大多数化合物是由5-氨基-4，6-二氯嘧啶经三步或6-氯嘌呤经烷基化两步制得。对MES的有效抗惊厥活性存在于在6-（甲氨基）-或6-（二甲氨基）嘌呤的9-位含有苄基取代基的化合物中。在控制癫痫发作的常用药物中，这种类型的结构代表了一类新的强效抗惊厥药物。
Several 9-alkyl-6-substituted purines were synthesized and tested for anticonvulsant activity against maximal electroshock-induced seizures (MES) in rats. Most compounds were prepared in three steps from 5-amino-4,6-dichloropyrimidine or in two steps via alkylation of 6-chloropurine. Potent anticonvulsant activity against MES resided in compounds that contain a benzyl substituent at the 9-position of 6-(methylamino)- or 6-(dimethylamino)purine. Among commonly used agents for control of seizures, this type of structure represents a new class of potent anticonvulsant agents.