1,3-Bispyridinium-dimethylether mono- and dioximes: synthesis, reactivating potency and therapeutic effect in experimental poisoning by organophosphorus compounds.

Abstract:

:Nine bispyridinium oximes containing two pyridinium rings linked by dimethylether were synthesised. Each compound had on one of the pyridinium rings a hydroxyiminomethyl group in position 2 or 4, while the other ring was unsubstituted or had a methyl or a hydroxyiminomethyl group in position 2 or 4. The reactivating potency and therapeutic effect of the oximes were tested on two organophosphates: O,O-dimethyl-2,2-dichlorovinylphosphate (DDVP) and O-ethyl-S-(2-diisopropylaminoethyl)-methylphosphonothioate (VX). The reactivation was measured on human erythrocyte acetylcholinesterase and the therapeutic effect was evaluated on male albino rats. The oximes with a hydroxyiminomethyl group in position 4 in the pyridinium ring were good reactivators of both phosphorylated and phosphonylated acetylcholinesterase. They were also very effective given together with atropine against VX and DDVP poisoning. The compounds are almost as effective as PAM-2, but PAM-2 is less toxic.

journal_name

Arch Toxicol

journal_title

Archives of toxicology

authors

Simeon V,Wilhelm K,Granov A,Besarović-Lazarev S,Buntić A,Fajdetić A,Binenfeld Z

doi

10.1007/BF00296900

subject

Has Abstract

pub_date

1979-02-23 00:00:00

pages

301-6

issue

4

eissn

0340-5761

issn

1432-0738

journal_volume

41

pub_type

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