• 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

潜在的乙酰胆碱酯酶复活剂:肟类和偕胺肟衍生物。

Potential acetylcholinesterase reactivators: oxime and amidoxime derivatives.

作者信息

Serafin B, Majewski M, Kleinrok Z, Jagiełło-Wojtowicz E, Rajtar G, Sieklucka-Dziuba M, Kolasa K

出版信息

Arch Immunol Ther Exp (Warsz). 1976;24(6):901-10.

PMID:1015993
Abstract

Out of 12 oximes and amidoximes (3 of which were new to the literature) the following showed a distinct antilethal effect in DFP poisoning: RA14 (1-methylbenzimidazole-2-aldoxime methiodide), RA14 (pyridine-4-aldoxime dodecyl bromide), and RA24 (pyridine-2-aldoxime dodecyl bromide). These compounds also reactivated acetylcholinesterase (AChE) in vitro, but had no effect on this enzyme in vivo. Moreover, addition of the dodecyl chain to pyridinealdoxtimes, or in a less degree replacement of the pyridine ring with benzimidazole in aldoximes, distinctly increased acute toxicity and lipophilicity when compared with the parent pyridine compounds, along with protective action in DFP poisoning.

摘要

在12种肟和偕胺肟(其中3种为文献中首次报道)中,以下几种在二异丙基氟磷酸酯(DFP)中毒时表现出明显的抗致死作用:RA14(1-甲基苯并咪唑-2-醛肟甲碘化物)、RA14(吡啶-4-醛肟十二烷基溴化物)和RA24(吡啶-2-醛肟十二烷基溴化物)。这些化合物在体外也能使乙酰胆碱酯酶(AChE)重新活化,但在体内对该酶无作用。此外,与母体吡啶化合物相比,在吡啶醛肟中添加十二烷基链,或在醛肟中用苯并咪唑较少程度地取代吡啶环,明显增加了急性毒性和亲脂性,同时在DFP中毒时有保护作用。

相似文献

1
Potential acetylcholinesterase reactivators: oxime and amidoxime derivatives.潜在的乙酰胆碱酯酶复活剂:肟类和偕胺肟衍生物。
Arch Immunol Ther Exp (Warsz). 1976;24(6):901-10.
2
In vitro oxime protection of human red blood cell acetylcholinesterase inhibited by diisopropyl-fluorophosphate.体外肟对二异丙基氟磷酸抑制的人红细胞乙酰胆碱酯酶的保护作用
J Appl Toxicol. 2008 May;28(4):422-9. doi: 10.1002/jat.1344.
3
Potential acetylcholinesterase reactivators: pyridine and alpha-oxooxime derivatives.潜在的乙酰胆碱酯酶复活剂:吡啶和α-氧代肟衍生物。
Pharmazie. 1986 Oct;41(10):699-702.
4
Antidotal efficacy of pyridinium chloride derivatives against soman poisoning.氯化吡啶鎓衍生物对梭曼中毒的解毒效果。
Basic Clin Pharmacol Toxicol. 2006 Jul;99(1):17-21. doi: 10.1111/j.1742-7843.2006.pto_385.x.
5
In vitro and in vivo evaluation of pyridinium oximes: mode of interaction with acetylcholinesterase, effect on tabun- and soman-poisoned mice and their cytotoxicity.吡啶肟类化合物的体外和体内评价:与乙酰胆碱酯酶的相互作用模式、对塔崩和梭曼中毒小鼠的影响及其细胞毒性。
Toxicology. 2006 Feb 15;219(1-3):85-96. doi: 10.1016/j.tox.2005.11.003. Epub 2005 Dec 5.
6
Cholinesterase reactivation in vivo with a novel bis-oxime optimized by computer-aided design.
J Pharmacol Exp Ther. 2003 Oct;307(1):190-6. doi: 10.1124/jpet.103.053405. Epub 2003 Jul 31.
7
Quaternary salts of 4,3' and 4,4' bis-pyridinium monooximes: synthesis and biological activity.
Bioorg Med Chem Lett. 2005 Jun 15;15(12):3076-80. doi: 10.1016/j.bmcl.2005.04.026.
8
Design, synthesis and biological evaluation of novel tetrahydroacridine pyridine- aldoxime and -amidoxime hybrids as efficient uncharged reactivators of nerve agent-inhibited human acetylcholinesterase.新型四氢吖啶吡啶-醛肟和-酰胺肟类化合物的设计、合成及作为非电活性化合物对神经毒剂抑制人乙酰胆碱酯酶的高效重活化剂的生物评价。
Eur J Med Chem. 2014 May 6;78:455-67. doi: 10.1016/j.ejmech.2014.03.044. Epub 2014 Mar 15.
9
An evaluation of therapeutic and reactivating effects of newly developed oximes (K156, K203) and commonly used oximes (obidoxime, trimedoxime, HI-6) in tabun-poisoned rats and mice.对新开发的肟类化合物(K156、K203)和常用肟类化合物(双复磷、氧磷定、HI-6)对塔崩中毒大鼠和小鼠的治疗及复活作用的评估。
Toxicology. 2008 Jan 20;243(3):311-6. doi: 10.1016/j.tox.2007.10.015. Epub 2007 Oct 26.
10
In vitro oxime reactivation of red blood cell acetylcholinesterase inhibited by methyl-paraoxon.甲基对硫磷抑制的红细胞乙酰胆碱酯酶的体外肟类复活作用
J Appl Toxicol. 2007 Mar-Apr;27(2):168-75. doi: 10.1002/jat.1189.