Design, synthesis, anticonvulsant activity, and pharmacophore study of new 1,5-diaryl-1H-1,2,4-triazole-3-carboxamide derivatives
1,5-Diaryl-1 H -1,2,4-triazole-3-carboxamide derivatives were designed, synthesized, and evaluated for its anticonvulsant activity using maximal electroshock (MES) and chemoshock (scPTZ and Strychnine) animal screen methods. Neurotoxicity was also assessed. In MES model, compound 4f showed 100% of p...
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Veröffentlicht in: | Medicinal chemistry research 2018-03, Vol.27 (3), p.928-938 |
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Hauptverfasser: | , , , , , |
Format: | Artikel |
Sprache: | eng |
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Online-Zugang: | Volltext |
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Zusammenfassung: | 1,5-Diaryl-1
H
-1,2,4-triazole-3-carboxamide derivatives were designed, synthesized, and evaluated for its anticonvulsant activity using maximal electroshock (MES) and chemoshock (scPTZ and Strychnine) animal screen methods. Neurotoxicity was also assessed. In MES model, compound
4f
showed 100% of phenytoin activity after both 0.5 and 4 h. In scPTZ model, compound
4e
showed 100% of sodium valproate activity. In Strychnine model, compound
4e
showed 120% more delay of onset of convulsion and 124% more delay of time of death relative to sodium valproate. Most of the target compounds showed mild neurotoxicity especially compound
4f
which showed excellent activity against electroshock. Pharmacophoric study reveals that the synthesized compounds showed good fitting on the pharmacophoric query with good RMSDX results. |
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ISSN: | 1054-2523 1554-8120 |
DOI: | 10.1007/s00044-017-2114-4 |