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Synthesis and in vitro evaluation of bis-quaternary 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide derivatives as reactivators against sarin and VX inhibited human acetylcholinesterase (hAChE).

Abstract：

:A series of bis-quaternary pyridinium derivatives 3a-3i of 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide (2) have been synthesized. The synthesized pyridinium compounds have an amide group in conjugation to the oxime moiety. These compounds were evaluated in vitro for their reactivation efficacy against organophosphorus (OP) nerve agents (NAs) (sarin and VX) inhibited human erythrocyte ghost acetylcholinesterase (hAChE) and compared with the reactivation efficacy of 2-PAM and obidoxime. The pKa values of the synthesized compounds were found closer to the pKa values of 2- and 4-pyridinium oxime reactivators such as 2-PAM and obidoxime. Some of the compounds have shown better reactivation efficacy than 2-PAM, and obidoxime against sarin and VX inhibited AChE.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Karade HN,Valiveti AK,Acharya J,Kaushik MP

doi

10.1016/j.bmc.2014.03.023

subject

Has Abstract

pub_date

2014-05-01 00:00:00

pages

2684-91

issue

9

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(14)00208-9

journal_volume

22

pub_type

杂志文章

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