In-vitro regeneration of sarin inhibited electric eel acetylcholinesterase by bis-pyridinium oximes bearing xylene linker

被引：14

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, Gwalior 474002, Madhya Pradesh, India

来源：

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY | 2009年 / 44卷 / 03期

关键词：

Bis-pyridinium oximes; Reactivators; 2-PAM; Organophosphorus nerve agents; Sarin; Acetylcholinesterase; Xylene linkers; BIOLOGICAL-ACTIVITY; QUATERNARY-SALTS; ACTIVE-CENTER; NERVE-GAS; MONOOXIMES; DIAGNOSIS;

D O I：

10.1016/j.ejmech.2008.02.020

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of bis-pyridinium oximes connected by xylene linker were synthesized and their in-vitro reactivation potential was evaluated against acetylcholinesterase (AChE) inhibited by nerve agent, sarin. Among the synthesized compounds, alpha,alpha'xylene-bis-[3,3'-(hydroxyimmomethyl) pyridinium] dibromide (3b) was found to be most potent reactivator for AChE inhibited by sarin. The oxime 3b exhibits 34% regeneration of inhibited AChE, in comparison to 20 and 15% regeneration by 2-PAM and obidoxime, respectively, at a concentration of 10(-4) M within 10 min. (C) 2008 Elsevier Masson SAS. All rights reserved.

引用

页码：1326 / 1330

页数：5

共 19 条

[1] In vitro reactivation of sarin inhibited electric eel acetylcholinesterase by bis-pyridinium oximes bearing methoxy ether linkages
Acharya, Jyotiranjan
Gupta, Arvind Kumar
Mazumder, Avik
Dubey, Devendra Kumar
TOXICOLOGY IN VITRO, 2008, 22 (02) : 525 - 530
[2] 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
[3] 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
[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] Synthesis and in vitro evaluation of xylene linked carbamoyl bis-pyridinium monooximes as reactivators of organophosphorus (OP) inhibited electric eel acetylcholinesterase (AChE)
Acharya, Jyotiranjan
Rana, Hemlata
Kaushik, M. P.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2011, 46 (09) : 3926 - 3933
[6] 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
[7] 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
[8] 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
[9] 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
[10] 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

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