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合成了5-取代-1,2,4-三唑并[4,3-a]喹唑啉衍生物2a～2q.利用最大电惊厥法(MES)和旋转棒法(Rotarod Test),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-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ED_(50)为19.7 mg/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-aminobutyric acid(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.
Synthesis of 5-substituted-1,2,4-triazolo [4,3-a] quinazoline derivatives 2a ~ 2q. Using the maximum electroconvulsive method (MES) and the Rotarod Test (Rotarod Test) The anticonvulsant activity and neurotoxicity were determined by intraperitoneal administration.The pharmacological results showed that the compound 5-n-heptyloxy-1,2,4-triazolo [4,3-a] quinazoline (2d ) Had the strongest anticonvulsant activity, the half effective dose was 19.7 mg / kg, and the protection index (PI) was 6.2. The anti-convulsive effect induced by chemicals showed that compound 2d could resist pentylenetetrazole, Hydrazine, thiosemicarbazide and 3-mercaptopropionic acid-induced convulsions, suggesting that its anticonvulsant effect is by enhancing the γ-aminobutyric acid (GABA) nervous system and activation of glutamic acid decarboxylase or GABA transaminase and anticonvulsant effect.