Monooxime reactivators of acetylcholinesterase with (E)-but-2-ene linker: preparation and reactivation of tabun- and paraoxon-inhibited acetylcholinesterase
Jazyk angličtina Země Anglie, Velká Británie Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
Grantová podpora
G0400930
Medical Research Council - United Kingdom
PubMed
17764957
DOI
10.1016/j.bmc.2007.08.002
PII: S0968-0896(07)00696-7
Knihovny.cz E-zdroje
- MeSH
- acetylcholinesterasa účinky léků MeSH
- antidota chemická syntéza chemie farmakologie MeSH
- cholinesterasové inhibitory otrava MeSH
- krysa rodu Rattus MeSH
- organofosfáty antagonisté a inhibitory farmakologie MeSH
- oximy chemická syntéza chemie farmakologie MeSH
- paraoxon antagonisté a inhibitory farmakologie MeSH
- racionální návrh léčiv MeSH
- reaktivátory cholinesterázy chemická syntéza chemie farmakologie MeSH
- vztahy mezi strukturou a aktivitou MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- acetylcholinesterasa MeSH
- antidota MeSH
- cholinesterasové inhibitory MeSH
- organofosfáty MeSH
- oximy MeSH
- paraoxon MeSH
- reaktivátory cholinesterázy MeSH
- tabun MeSH Prohlížeč
Acetylcholinesterase reactivators are crucial antidotes for the treatment of organophosphate intoxication. Fifteen new monooxime reactivators of acetylcholinesterase 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.
Citace poskytuje Crossref.org
Novel Group of AChE Reactivators-Synthesis, In Vitro Reactivation and Molecular Docking Study
