3,3'-联吡啶单肟作为有机磷中毒的解毒剂。

The 3,3'-bis-pyridinium mono-oximes as antidotes against organophosphorous intoxication.

作者信息

Sikder A K, Pandey K S, Jaiswal D K, Dube S N, Kumar D, Husain K, Bhattacharya R, Das Gupta S

机构信息

Synthetic Chemistry Division, Defence Research & Development Establishment, Gwalior, India.

出版信息

J Pharm Pharmacol. 1992 Dec;44(12):1038-40.

PMID:1361555

Abstract

In an attempt to develop effective antidotes against organophosphorous intoxication, three new structurally related bispyridinium mono-oximes with a 2-oxopropane bridge were synthesized. The compounds were evaluated for in-vivo therapeutic protection and cholinesterase reactivation in blood and various brain regions. In neuromuscular function studies against diisopropyl-fluorophosphate and isopropyl methylphosphonofluoridate poisoning, the oximes produced significant protection. The compounds produced marked peripheral reactivation and beneficial effects on neuromuscular transmission. The reactivation of cholinesterase in cerebral cortex by the oximes, in spite of their being quaternary salts is a notable feature.

摘要

为了研发针对有机磷中毒的有效解毒剂，合成了三种新的具有2-氧代丙烷桥的结构相关的双吡啶单肟。对这些化合物进行了体内治疗保护以及血液和各个脑区胆碱酯酶复活作用的评估。在针对二异丙基氟磷酸酯和甲基异丙基膦酸氟化物中毒的神经肌肉功能研究中，这些肟产生了显著的保护作用。这些化合物产生了明显的外周复活作用以及对神经肌肉传递的有益影响。尽管这些肟是季铵盐，但它们能使大脑皮层中的胆碱酯酶复活，这是一个显著的特点。