54506-04-6Relevant articles and documents
Design, synthesis, anticonvulsant activity, and pharmacophore study of new 1,5-diaryl-1H-1,2,4-triazole-3-carboxamide derivatives
Abuelhassan, Abdelfattah H.,Badran, Mostafa M.,Hassan, Heba A.,Abdelhamed, Dalia,Elnabtity, Sameh,Aly, Omar M.
, p. 928 - 938 (2017/11/27)
1,5-Diaryl-1H-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.
Process for the manufacture of 2-phenyl-4,5-oxazoledione 4-phenylhydrazone derivatives
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, (2008/06/13)
A process for manufacturing derivatives of 2-phenyl-4,5-oxazoledione 4-phenylhyrazone is disclosed. The process comprises reacting a derivative of a benezenediazonium salt, a hippuric acid derivative, and acetic anhydride in the presence of a neutralizing agent to effect the cyclization reaction for the formation of the oxazolone ring and the succeeding diazo-coupling reaction. The process does not require the conventional separate, independent step for the preparation of a solution of a hippuric acid derivative and acetic anhydride, thus eliminating the quick heating and quenching procedures and further avoiding the loss of the hippuric acid derivative due to decomposition of the oxazolone derivative. There is thus obtained a high yield of the desired product in a short period of time.
