Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 15, Issue 21, Pages 6733-6741Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2007.08.002
Keywords
acetylcholinesterase; reactivation; nerve agent; tabun pesticide; paraoxon; reactivator; oxime
Funding
- Medical Research Council [G0400930] Funding Source: researchfish
- MRC [G0400930] Funding Source: UKRI
- Medical Research Council [G0400930] Funding Source: Medline
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Acetylcholinesterase reactivators are crucial antidotes for the treatment of organophosphate intoxication. Fifteen new monooxime reactivators of acetyleholinesterase with a (E)-but-2-ene linker were developed in an effort to extend the properties of K-oxime (E)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide (K203). The known reactivators (pralidoxime, HI-6, obidoxime, K075, K203) and the new compounds were tested in vitro on a model of tabun- and paraoxon-inhibited AChE. Monooxime reactivators were not able to exceed the best known compounds for tabun poisoning, but some of them did show reactivation comparable with known compounds for paraoxon poisoning. However, extensive differences were found by a SAR study for various substitutions on the non-oxime part of the reactivator molecule. (C) 2007 Elsevier Ltd. All rights reserved.
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