• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

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.

DOI:10.1016/j.ejmech.2005.12.003
PMID:16472891
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。

相似文献

1
Synthesis of some new substituted triazolo [4,3-a][1,4] benzodiazepine derivatives as potent anticonvulsants.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。
Eur J Med Chem. 2006 Mar;41(3):417-22. doi: 10.1016/j.ejmech.2005.12.003. Epub 2006 Feb 10.
2
Synthesis of some quinoline-2(1H)-one and 1, 2, 4 - triazolo [ 4 , 3 -a ] quinoline derivatives as potent anticonvulsants.一些喹啉-2(1H)-酮和1,2,4-三唑并[4,3-a]喹啉衍生物作为强效抗惊厥剂的合成。
J Pharm Pharm Sci. 2007;10(3):254-62.
3
Synthesis and evaluation of pharmacological properties of novel annelated 2,3-benzodiazepine derivatives.新型稠合2,3-苯并二氮杂䓬衍生物的合成及其药理性质评价
J Med Chem. 2003 Aug 14;46(17):3758-61. doi: 10.1021/jm030821p.
4
Synthesis of some new 4-styryltetrazolo[1,5-a]quinoxaline and 1-substituted-4-styryl[1,2,4]triazolo[4,3-a]quinoxaline derivatives as potent anticonvulsants.一些新型4-苯乙烯基四唑并[1,5-a]喹喔啉和1-取代-4-苯乙烯基[1,2,4]三唑并[4,3-a]喹喔啉衍生物作为强效抗惊厥剂的合成。
Eur J Med Chem. 2009 Mar;44(3):1135-43. doi: 10.1016/j.ejmech.2008.06.006. Epub 2008 Jun 20.
5
Synthesis and pharmacological activity of 1,4-benzodiazepine derivatives.1,4-苯二氮䓬衍生物的合成及药理活性
Boll Chim Farm. 2002 Jan-Feb;141(1):8-14.
6
Novel fused 1,2,3-triazolo-benzodiazepine derivatives as potent anticonvulsant agents: design, synthesis, in vivo, and in silico evaluations.新型融合 1,2,3-三唑并苯并二氮杂䓬衍生物作为有效的抗惊厥药物:设计、合成、体内和计算评估。
Mol Divers. 2020 Feb;24(1):179-189. doi: 10.1007/s11030-019-09940-9. Epub 2019 Mar 20.
7
Evaluation of antimycobacterial and anticonvulsant activities of new 1-(4-fluorobenzoyl)-4-substituted-thiosemicarbazide and 5-(4-fluorophenyl)-4-substituted-2,4-dihydro-3H-1,2,4-triazole-3-thione derivatives.新型1-(4-氟苯甲酰基)-4-取代硫代氨基脲和5-(4-氟苯基)-4-取代-2,4-二氢-3H-1,2,4-三唑-3-硫酮衍生物的抗分枝杆菌和抗惊厥活性评价
Farmaco. 1997 Nov;52(11):691-5.
8
Synthesis, anticonvulsant and toxicity evaluation of 2-(1H-indol-3-yl)acetyl-N-(substituted phenyl)hydrazine carbothioamides and their related heterocyclic derivatives.2-(1H-吲哚-3-基)乙酰基-N-(取代苯基)肼基硫代甲酰胺及其相关杂环衍生物的合成、抗惊厥活性及毒性评价
Acta Pharm. 2008 Dec;58(4):445-54. doi: 10.2478/v10007-008-0025-0.
9
Synthesis and preliminary screening of benzothiazol-2-yl thiadiazole derivatives for anticonvulsant activity.合成及初步筛选苯并噻唑-2-基噻二唑衍生物的抗惊厥活性。
Acta Pharm. 2009 Dec;59(4):441-51. doi: 10.2478/v10007-009-0031-x.
10
Synthesis and potential anticonvulsant activity of new N-3-substituted 5,5-cyclopropanespirohydantoins.新型N-3-取代的5,5-环丙烷螺乙内酰脲的合成及其潜在的抗惊厥活性
Eur J Med Chem. 2009 Jan;44(1):296-302. doi: 10.1016/j.ejmech.2008.02.024. Epub 2008 Mar 7.

引用本文的文献

1
Phytochemical Constituents of L. (Baobab) Fruit Pulp from Tekeze Valley, Tigrai, Ethiopia.埃塞俄比亚提格雷州特克泽河谷的巴氏猴面包树果实果肉的植物化学成分
Int J Anal Chem. 2023 Oct 25;2023:5591059. doi: 10.1155/2023/5591059. eCollection 2023.
2
Novel fused 1,2,3-triazolo-benzodiazepine derivatives as potent anticonvulsant agents: design, synthesis, in vivo, and in silico evaluations.新型融合 1,2,3-三唑并苯并二氮杂䓬衍生物作为有效的抗惊厥药物:设计、合成、体内和计算评估。
Mol Divers. 2020 Feb;24(1):179-189. doi: 10.1007/s11030-019-09940-9. Epub 2019 Mar 20.
3
Recent developments on triazole nucleus in anticonvulsant compounds: a review.
抗惊厥化合物中三唑核的最新进展:综述
J Enzyme Inhib Med Chem. 2018 Dec;33(1):453-478. doi: 10.1080/14756366.2017.1423068.