Assessment of antidotal efficacy of cholinesterase reactivators against paraoxon: In vitro reactivation kinetics and physicochemical properties

Result code in IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00179906%3A_____%2F14%3A10281225" target="_blank" >RIV/00179906:_____/14:10281225 - isvavai.cz</a>

Alternative codes found

RIV/62690094:18470/14:50002647

Result on the web

<a href="http://www.sciencedirect.com/science/article/pii/S0960894X14008300" target="_blank" >http://www.sciencedirect.com/science/article/pii/S0960894X14008300</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.bmcl.2014.07.095" target="_blank" >10.1016/j.bmcl.2014.07.095</a>

Result language

angličtina

Original language name

Assessment of antidotal efficacy of cholinesterase reactivators against paraoxon: In vitro reactivation kinetics and physicochemical properties

Original language description

The search of proficient oximes as reactivators of irreversibly inhibited-AChE by organophosphate poisoning necessitates an appropriate assessment of their physicochemical properties and reactivation kinetics. Therefore, herein acid dissociation constant; pKa, lipophilicity; logP, polar surface area, hydrogen bond donor and acceptor counts of structurally different oximes (two tertiary oximes and thirteen pyridinium aldoxime derivatives) have been evaluated. The experimentally obtained data for pKa hasbeen comparatively analyzed by using non-linear regression. Further the tested oximes were screened through in vitro reactivation kinetics against paraoxon-inhibited AChE. The pKa values of all the examined oximes were within the range of 7.50-9.53. pKavalues of uncharged and mono-pyridinium oximes were in good correlation with their reactivation potency. The high negative logP values of pyridinium oxime reactivators indicate their high hydrophilic character; hence oximes with improved

Czech name

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Czech description

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Type

J_x - Unclassified - Peer-reviewed scientific article (Jimp, Jsc and Jost)

CEP classification

FR - Pharmacology and apothecary chemistry

OECD FORD branch

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Project

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Continuities

I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Publication year

2014

Confidentiality

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Name of the periodical

Bioorganic and Medicinal Chemistry Letters

ISSN

0960-894X

e-ISSN

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Volume of the periodical

24

Issue of the periodical within the volume

19

Country of publishing house

GB - UNITED KINGDOM

Number of pages

6

Pages from-to

4743-4748

UT code for WoS article

000342574600024

EID of the result in the Scopus database

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