A series of 3-[(4-substituted-benzylidene)-amino]-2-phenyl-3H-quinazolin-4-ones (5a-k) were synthesized by reacting 3-amino-2-phenyl-1H-quinazolin-4-one with p-hydroxybenzaldehyde, and then further with various alkyl/benzyl halides or substituted phenacyl bromides. The structures of the compounds were confirmed on the basis of IR, NMR, MS and elemental analysis. Anticonvulsant activities were evaluated using the MES and scPTZ tests. Some of the selected compounds were evaluated for antidepressant activity by forced swim pool test. Compound 3-[(4-butoxy-benzylidene)-amino]-2-phenyl-3H-quinazolin-4-one was emerged as the most promising anticonvulsant agent without any motor impairment effect. The whole brain GABA estimation of brain homogenate indicated that the anticonvulsant activity of above mentioned quinazolinone derivatives might be due to an increased GABA concentration.

译文

通过与对羟基苯甲醛反应3-amino-2-phenyl-1H-quinazolin-4-one,然后与各种烷基/苄基卤化物或取代的苯基溴化物进一步反应,合成了一系列3-[(4-取代-亚苄基)-氨基]-2-苯基-3h-喹唑啉-4-酮 (5a-k)。根据IR,NMR,MS和元素分析确定了化合物的结构。使用MES和scPTZ测试评估抗惊厥活性。通过强制游泳池测试评估了某些选定化合物的抗抑郁活性。化合物3-[(4-丁氧基-亚苄基)-氨基]-2-苯基-3h-喹唑啉-4-酮被认为是最有前途的抗惊厥剂,没有任何运动障碍作用。脑匀浆的全脑GABA估计表明,上述喹唑啉酮衍生物的抗惊厥活性可能是由于GABA浓度增加所致。

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