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一些新型取代三唑并[4,3-a][1,4]苯二氮䓬衍生物作为强效抗惊厥剂的合成。

Synthesis of some new substituted triazolo [4,3-a][1,4] benzodiazepine derivatives as potent anticonvulsants.

作者信息

Narayana B, Vijaya Raj K K, Ashalatha B V, Kumari N Suchetha

机构信息

Department of Post-Graduate Studies and Research in Chemistry, Mangalore University, Mangalagangotri, India.

出版信息

Eur J Med Chem. 2006 Mar;41(3):417-22. doi: 10.1016/j.ejmech.2005.12.003. Epub 2006 Feb 10.

Abstract

Novel 8-chloro-6-(2-fluorophenyl)-1-(aryl)-4H-[1,2,4]triazolo[4,3-a][1,4]benzodiazepines (5a-f) were prepared by treating 7-chloro-5-(2-fluorophenyl)-1,3-dihydro-2H-1,4-benzodiazepine-2-thione with various aromatic acid hydrazides. The newly prepared compounds were characterized by spectral analysis. Compounds were tested for anticonvulsant activity. Four of the tested compounds such as 5a, 5d, 5e and 5f exhibited excellent anticonvulsant activity in comparison with standard drug, diazepam.

摘要

通过用各种芳香族酰肼处理7-氯-5-(2-氟苯基)-1,3-二氢-2H-1,4-苯并二氮杂卓-2-硫酮,制备了新型的8-氯-6-(2-氟苯基)-1-(芳基)-4H-[1,2,4]三唑并[4,3-a][1,4]苯并二氮杂卓(5a-f)。通过光谱分析对新制备的化合物进行了表征。对化合物进行了抗惊厥活性测试。与标准药物地西泮相比,所测试的四种化合物,如5a、5d、5e和5f,表现出优异的抗惊厥活性。

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