Synthesis and Anticonvulsant Activity Evaluation of 3-alkoxy-4-(4-(hexyloxy/heptyloxy)phenyl)-4<i>H</i>-1,2,4 -triazole

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AuthorYing-Quan Fangen
AuthorChun-Ling Sunen
AuthorDa-Chuan Liuen
AuthorShi-Ben Wangen
AuthorZhe-San Quanen
Issued Date2015-01-31en
AbstractA series of 3-alkoxy-4-(4-(hexyloxy/heptyloxy) phenyl)-4H-1,2,4-triazole was synthesized. The anticonvulsant effect and neurotoxicity of the compounds were calculated with maximal electroshock (MES) test and rotarod tests with intraperitoneally injected mice. Among the synthesized compounds, compound 3-heptyloxy-4-(4-(hexyloxy) phenyl)-4H-1,2,4-triazole (5f) was the most active one and also had the lowest toxicity. In the anti-MES potency test, it showed median effective dose (ED50) of 37.3 mg/Kg, median toxicity dose (TD50) of 422.5 mg/Kg, and the protective index (PI) of 11.3 which is much greater than the reference drug carbamazepine with PI value of 6.4. As well as demonstrating the anti-MES efficacy of compound 5f, its potency against seizures induced by pentylenetetrazole, 3-mercaptopropionic acid, and bicuculline were also established, with the results suggesting that GABA-mediated mechanisms might be involved in its anticonvulsant activity, such as enhancing of GABAergic neurotransmission or activity, activate GAD or inhibit GABA-T, and GABAA-mediated mechanisms.en
DOIhttps://doi.org/10.22037/ijpr.2015.1623en
KeywordSynthesisen
KeywordTriazoleen
KeywordTriazoloneen
KeywordAnticonvulsant activityen
KeywordNeurotoxicityen
KeywordPentylenetetrazoleen
Keyword3-Mercaptopropionic aciden
KeywordBicucullineen
PublisherBrieflandsen
TitleSynthesis and Anticonvulsant Activity Evaluation of 3-alkoxy-4-(4-(hexyloxy/heptyloxy)phenyl)-4<i>H</i>-1,2,4 -triazoleen
TypeOriginal Articleen

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