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Synthesis and Anticonvulsant Activity of 1-Formamide-triazolo[4,3-a]quinoline Derivatives
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  • Synthesis and Anticonvulsant Activity of 1-Formamide-triazolo[4,3-a]quinoline Derivatives
  • Synthesis and Anticonvulsant Activity of 1-Formamide-triazolo[4,3-a]quinoline Derivatives
저자명
Wei. Cheng-Xi,Deng. Xian-Qing,Chai. Kyu-Yun,Sun. Zhi-Gang,Quan. Zhe-Shan
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
2010년|33권 5호|pp.655-662 (8 pages)
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정기간행물|ENG|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

Using 6-hydroxy-3,4-dihydro-2(1H)-quinolone as the starting material, a series of 1-formamide-triazolo[4, 3-a]quinoline derivatives (6a-6n) was synthesized, the anticonvulsant effect and neurotoxicity of the compounds was calculated with maximal electroshock test and rotarod tests with intraperitoneally injected in KunMing mice. The results demonstrated that compound 7-(hexyloxy)-4,5-dihydro-[1,2,4] triazolo[4,3-${alpha}$]quinoline-1-carboxamide (6d) was the most active one and also had the lowest toxicity. In the anti-maximal electroshock potency test, it showed median effective dose ($ED_{50}$) of 30.1 mg/kg, median toxicity dose ($TD_{50}$) of 286 mg/kg, and the protective index of 9.5 which is greater than the reference drug carbamazepine with the protective index value of 6.0.