In vitro reactivation of organophosphorus (OP)-inhibited electric eel acetylcholinesterase by novel monoquaternary pyridinium oximes

被引：7
|
作者：
Acharya, Jyotiranjan [1 ]
Rana, Hemlata [1 ]
Kapil, V. Aditya [1 ]
Kaushik, M. P. [1 ]
机构：
[1] Def Res & Dev Estab, Proc Technol Dev Div, Gwalior 474002, India
来源：
MEDICINAL CHEMISTRY RESEARCH | 2013年 / 22卷 / 03期
关键词：
Pyridinium oximes; Reactivators; 2-PAM; Acetylcholinesterase; Organophosphorus inhibitors; ACTIVE-CENTER; EFFICACY; PESTICIDES; DIAGNOSIS; MECHANISM; POTENCY; LINKER; DESIGN; SERIES;
D O I：
10.1007/s00044-012-0128-5
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The synthesis of a series of monoquaternary pyridinium oximes bearing either a long-chain alkyloxymethyl or benzyloxymethyl side chain and the corresponding in vitro evaluation for the reactivation of electric eel acetylcholinesterase-inhibited organophosphorus inhibitors viz. sarin, DFP, and VX is reported. The data were compared with that of 2-PAM and obidoxime. Compounds bearing a benzyloxymethyl and 4-methylbenzyloxymethyl side chain showed better reactivation compared to obidoxime. However, none of the newly synthesized oximes bearing an aliphatic side chain could surpass the reactivation potential of 2-PAM. The pKa of the new oximes were determined and correlated with the observed reactivation potential.
引用
收藏
页码：1277 / 1286
页数：10
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