茶碱并四唑类衍生物的设计合成以及抗惊厥活性的研究  

Design,Synthesis and Anticonvulsant Evaluation of Theophylline Containing Tetrazole Derivates

作　　者：全殷晟 金光浩[1] 尹秀梅[1] 全哲山[1] 

机构地区：[1]延边大学药学院药物化学教研室

出　　处：《化学试剂》2018年第1期17-20,共4页Chemical Reagents

摘　　要：寻找高效的潜在抗癫痫药物,设计合成系列目标化合物并测定其抗惊厥活性。以8-氯茶碱为起始原料,经取代、肼代和环合3步反应合成目标化合物,并采用最大电惊厥法对所合成化合物进行抗惊厥活性的测定。所有合成化合物结构经^1HNMR和^13CNMR进行确证。其中,4-正壬烷-6,8-二甲基-4H-苯并[4,5]咪唑并[1,2-d]四唑-5,7（6H,8H）-二酮的抗惊厥活性最强,其ED50为22.38 mg/kg,具有潜在的抗癫痫活性。Objective searching for novel high efficiency anticonvulsant active substances,a series of 4-substituted-6,8-dimethyl-4 H-benzo[4,5]imidazo[1,2-d]tetrazole-5,7（6H,8H）-dione derivatives were designed,synthesized and evaluated for their anticonvulsant activity.8-Chloro-1,3-dimethyl-2,6-（1H,3H）-purinedione as a starting material,the target compounds were prepared via displacement reaction and cyclization reaction,and their anticonvulsant activity were investigated by the maximal electroshock seizure.The structures of synthesized compounds were confirmed by ^1HNMR and ^13CNMR.The compound 4-nonyl-6,8-dimethyl-4H-benzo[4,5]imidazo[1,2-d]tetrazole-5,7（6H,8H）-dione showed the most anticonvulsant activity with ED（50） values of 22.38 mg/kg,as a potential antiepileptic activity.

关 键 词：茶碱 四唑 合成 抗惊厥活性 最大电惊厥 

分 类 号：R914.5[医药卫生—药物化学]