中文摘要：

合成了5-取代-1，2，4-三唑并[4，3-1]喹唑啉衍生物2a-2q．利用最大电惊厥法（MEs）和旋转棒法（RotarodTest），以小鼠腹腔给药，分别测定了其抗惊厥活性和神经毒性．药理实验结果表明，化合物5一正庚氧基-1，2，4-三唑并[4，3-a]喹唑啉（2d）的抗惊厥活性最强，其半数有效量ED50为19．7mg／kg，保护指数PI为6．2-由化学物质诱发的抗惊厥实验结果表明，化合物2d能对抗由戊四唑、异烟肼、硫代氨基脲和3-巯基丙酸诱发的惊厥作用，推测其抗惊厥作用是通过增强γ-aminobutyricacid（GABA）神经能系统和活化谷氨酸脱羧酶或抑制GABA转氨酶而起抗惊厥作用．

英文摘要：

A series of 5-substituted-[1,2,4]triazolo[4,3-a]quinazolines were synthesized. The anticonvulsant effects and neurotoxicity of the compounds were evaluated with maximal electroshock test and rotarod test with intraperitoneally injected in mice. The pharmacology results showed that 5-pentyloxy-[1,2,4]triazolo- [4,3-a]quinazoline （2d） was the most potent with EDso value of 19.7 mg/kg and protective index （PI= TD50/EDs0） value of 6.2. To explain the possible mechanism of anticonvulsant activity, compound 2d was tested in several chemical induced seizures tests. The results revealed that compound 2d was effective against the seizures induced by pentylenetetrazole, isoniazid, 3-mercaptopropionic acid and thiosemicarba- zide, which suggested that the anticonvulsant effects of this series compounds were acted via increasing y-aminobutyric acid （GABA） ergic neurotransmission and activating glutamate decarboxylase （GAD） or in- hibiting a-oxoglutarate aminotransferase （GABA-T） in the brain.