In vitro reactivation of sarin inhibited electric eel acetylcholinesterase by bis-pyridinium oximes bearing methoxy ether linkages

被引:21
|
作者
Acharya, Jyotiranjan [1 ]
Gupta, Arvind Kumar [1 ]
Mazumder, Avik [1 ]
Dubey, Devendra Kumar [1 ]
机构
[1] Def Res & Dev Estab, Proc Technol Dev Div, Jhansi Rd, Gwalior 474002, India
关键词
bis-pyridinium oximes; reactivators; 2-PAM; sarin; nerve agents; acetylcholinesterase; obidoxime;
D O I
10.1016/j.tiv.2007.10.006
中图分类号
R99 [毒物学(毒理学)];
学科分类号
100405 ;
摘要
Bis-pyridinium oximes connected by methoxy alkane ether linker were synthesized and their in vitro reactivation efficacy was evaluated for sarin inhibited ACNE. Reactivation efficacy of synthesized compounds was compared with 2-PAM and obidoxime. Among the synthesized compounds, 1,2-dimethoxy ethylene bis-[3,3'-(hydroxyiminomethyl) pyridinium] dichloride (3P-2) and 1,3-dimethoxy propylene bis-[3,3'-(hydroxyiminomethyl) pyridinium] dichloride (3P-3) were found to be most potent reactivators for AChE inhibited by nerve agent sarin. 3P-2 and 3P-3, respectively exhibited 80% and 69% regeneration of inhibited ACNE, whereas 2-PAM (well known antidote for nerve agent poisoning) showed 42% regeneration. (C) 2007 Elsevier Ltd. All rights reserved.
引用
下载
收藏
页码:525 / 530
页数:6
相关论文
共 22 条
  • [1] In-vitro regeneration of sarin inhibited electric eel acetylcholinesterase by bis-pyridinium oximes bearing xylene linker
    Acharya, Jyotiranjan
    Gupta, Arvind Kumar
    Mazumder, Avik
    Dubey, Devendra Kumar
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (03) : 1326 - 1330
  • [2] In vitro reactivation potency of novel symmetrical bis-pyridinium oximes for electric eel acetylcholinesterase inhibited by nerve agent sarin
    Acharya, Jyotiranjan
    Dubey, Devendra Kumar
    Kaushik, M. P.
    TOXICOLOGY IN VITRO, 2011, 25 (08) : 2135 - 2139
  • [3] In vitro evaluation of bis-pyridinium oximes bearing methoxy alkane linker as reactivators of sarin inhibited human acetylcholinesterase
    Acharya, Jyotiranjan
    Dubey, Devendra Kumar
    Raza, Syed Kalbey
    TOXICOLOGY IN VITRO, 2010, 24 (06) : 1797 - 1802
  • [4] In vitro reactivation of sarin-inhibited human acetylcholinesterase (AChE) by bis-pyridinium oximes connected by xylene linkers
    Acharya, Jyotiranjan
    Dubey, Devendra Kumar
    Srivastava, Ashish Kumar
    Raza, Syed Kalbey
    TOXICOLOGY IN VITRO, 2011, 25 (01) : 251 - 256
  • [5] In vitro reactivation of organophosphorus (OP)-inhibited electric eel acetylcholinesterase by novel monoquaternary pyridinium oximes
    Jyotiranjan Acharya
    Hemlata Rana
    V. Aditya Kapil
    M. P. Kaushik
    Medicinal Chemistry Research, 2013, 22 : 1277 - 1286
  • [6] In vitro reactivation of organophosphorus (OP)-inhibited electric eel acetylcholinesterase by novel monoquaternary pyridinium oximes
    Acharya, Jyotiranjan
    Rana, Hemlata
    Kapil, V. Aditya
    Kaushik, M. P.
    MEDICINAL CHEMISTRY RESEARCH, 2013, 22 (03) : 1277 - 1286
  • [7] In vitro reactivation kinetics of paraoxon- and DFP-inhibited electric eel AChE using mono- and bis-pyridinium oximes
    Gupta, Bhanushree
    Sharma, Rahul
    Singh, Namrata
    Kuca, Kamil
    Acharya, J. R.
    Ghosh, Kallol K.
    ARCHIVES OF TOXICOLOGY, 2014, 88 (02) : 381 - 390
  • [8] In vitro reactivation kinetics of paraoxon- and DFP-inhibited electric eel AChE using mono- and bis-pyridinium oximes
    Bhanushree Gupta
    Rahul Sharma
    Namrata Singh
    Kamil Kuca
    J. R. Acharya
    Kallol K. Ghosh
    Archives of Toxicology, 2014, 88 : 381 - 390
  • [9] REACTIVATION OF SARIN-PHOSPHONYLATED OR SOMAN-PHOSPHONYLATED HUMAN ACETYLCHOLINESTERASE BY BIS-PYRIDINIUM MONO-OXIMES
    SUN, MC
    LI, FZ
    CHOU, TC
    BIOCHEMICAL PHARMACOLOGY, 1986, 35 (02) : 347 - 349
  • [10] Synthesis and evaluation of novel bis-pyridinium oximes as reactivators of DFP-inhibited acetylcholinesterase
    Acharya, Jyotiranjan
    Gupta, Arvind Kumar
    Dubey, Devendra Kumar
    Raza, Syed Kalbey
    EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2009, 44 (03) : 1335 - 1340