Synthesis of 2-substituted-7-heptyloxy-4,5-dihydro-(1,2,4)-triazolo(4,3-a)quinolin-1(2H)-ones with anticonvulsant activity.

Wei CX; Li FN; Zhao LX; Zhao LM; Quan ZS

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Synthesis of 2-substituted-7-heptyloxy-4,5-dihydro-(1,2,4)-triazolo(4,3-a)quinolin-1(2H)-ones with anticonvulsant activity.

机译：具有抗惊厥活性的2-取代-7-庚氧基-4,5-二氢-（1,2,4）-三唑并（4,3-a）喹啉-1（2H）-的合成。

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A series of 2-substituted-7-heptyloxy-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinolin-1(2H)-ones was synthesized. The anticonvulsant effect and neurotoxicity of the compounds were calculated with maximal electroshock (MES) test, subcutaneous pentylenetetrazole (sc-PTZ), and rotarod tests with intraperitoneally injected mice. Among the synthesized compounds, 2-propionyl-7-heptyloxy-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoline-1(2H)-one 4b was the most active one and also had the lowest toxicity. In the anti-MES potency test, it showed median effective dose (ED(50)) of 8.2 mg/kg, median toxicity dose (TD(50)) of 318.3 mg/kg, and the protective index (PI) of 39.0 which is much greater than the PI of the reference drugs phenytoin and carbamazepine.

机译：合成了一系列2-取代的-7-庚氧基-4,5-二氢-[1,2,4]三唑并[4,3-a]喹啉-1（2H）-one。化合物的抗惊厥作用和神经毒性通过最大电击（MES）试验，皮下戊烯四唑（sc-PTZ）和腹膜内注射小鼠的rotarod试验进行计算。在合成的化合物中，2-丙酰基-7-庚氧基-4,5-二氢-[1,2,4]三唑并[4,3-a]喹啉-1（2H）-一个4b是活性最高的化合物，毒性最低。在抗MES效能测试中，中位有效剂量（ED（50））为8.2 mg / kg，中位毒性剂量（TD（50））为318.3 mg / kg，保护指数（PI）为39.0，比参考药物苯妥英和卡马西平的PI值大得多。

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《Archiv der Pharmazie》 |2007年第9期|共5页
作者
Wei CX; Li FN; Zhao LX; Zhao LM; Quan ZS;
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正文语种 eng
中图分类药学;
关键词
Animals; Anticonvulsants; Mice; Quinolones; Structure-Activity Relationship; 动物; 抗惊厥药; 小鼠; 喹诺酮类; 构效关系;

机译：Animals;Anticonvulsants;Mice;Quinolones;Structure-Activity Relationship;动物;抗惊厥药;小鼠;喹诺酮类;构效关系;

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1. Synthesis of 2-substituted-7-heptyloxy-4,5-dihydro-(1,2,4)-triazolo(4,3-a)quinolin-1(2H)-ones with anticonvulsant activity. [J] . Wei CX, Li FN, Zhao LX, Archiv der Pharmazie . 2007,第9期

机译：具有抗惊厥活性的2-取代-7-庚氧基-4,5-二氢-（1,2,4）-三唑并（4,3-a）喹啉-1（2H）-的合成。
2. Synthesis and anticonvulsant activity of 1-substituted-7-benzyloxy-4,5-dihydro-(1,2,4)triazolo(4,3-a)quinoline. [J] . Cui LJ, Xie ZF, Piao HR, Biological & pharmaceutical bulletin . 2005,第7期

机译：1-取代-7-苄氧基-4,5-二氢-（1,2,4）三唑并（4,3-a）喹啉的合成及抗惊厥活性
3. Design and synthesis of 5-alkoxy-(1,2,4)triazolo(4,3-a)quinoline derivatives with anticonvulsant activity. [J] . Guo LJ, Wei CX, Jia JH, European Journal of Medicinal Chemistry: Chimie Therapeutique . 2009,第3期

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4. Synthesis of the 3,6-dinitro-1,2,4triazolo 4,3-b1,2,4triazolate anion and characterization of its energetic salts [C] . Matthew Gettings, Matthias Zeller, Edward Byrd, Seminar on new trends in research of energetic materials . 2020

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Synthesis of 2-substituted-7-heptyloxy-4,5-dihydro-(1,2,4)-triazolo(4,3-a)quinolin-1(2H)-ones with anticonvulsant activity.

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