芳基氨基脲的氨基脲模板环化反应：4,5-二苯基-2H-1,2,4-三唑-3(4H)-酮的合成与抗惊厥活性

Cyclization of the semicarbazone template of aryl semicarbazones: synthesis and anticonvulsant activity of 4,5-diphenyl-2H-1,2,4-triazol-3(4H)-one.

作者信息

Shalini M, Yogeeswari P, Sriram D, Stables J P

机构信息

Medicinal Chemistry Research Laboratory, Pharmacy Group, Birla Institute of Technology and Science, 333031 Pilani, India

出版信息

Biomed Pharmacother. 2009 Mar;63(3):187-93. doi: 10.1016/j.biopha.2006.04.002.

DOI:10.1016/j.biopha.2006.04.002

PMID:19422088

Abstract

A new series of 4,5-diphenyl-2H-1,2,4-triazol-3(4H)-one were synthesized to study the effect of cyclization of the semicarbazone moiety of aryl semicarbazones on the anticonvulsant activity. Structures of the synthesized compounds were confirmed by the use of their spectral data besides elemental analysis. All compounds were evaluated for their anticonvulsant activity in four animal models of seizures, viz. maximal electroshock seizure (MES), subcutaneous pentylenetetrazole (scPTZ), subcutaneous strychnine (scSTY), and subcutaneous picrotoxin (scPIC)-induced seizure threshold tests. The compounds were also evaluated for neurotoxicity. Compounds 4, 9, 14-19 exhibited anticonvulsant activity in all the four animal models of seizure.

摘要

合成了一系列新的4,5-二苯基-2H-1,2,4-三唑-3(4H)-酮，以研究芳基氨基脲的氨基脲部分环化对抗惊厥活性的影响。除了元素分析外，还利用光谱数据确认了合成化合物的结构。在四种癫痫动物模型中评估了所有化合物的抗惊厥活性，即最大电休克惊厥（MES）、皮下注射戊四氮（scPTZ）、皮下注射士的宁（scSTY）和皮下注射印防己毒素（scPIC）诱导的惊厥阈值测试。还评估了这些化合物的神经毒性。化合物4、9、14 - 19在所有四种癫痫动物模型中均表现出抗惊厥活性。