Synthesis of the novel series of bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against chlorpyrifos-inhibited acetylcholinesterase
Jazyk angličtina Země Anglie, Velká Británie Médium print-electronic
Typ dokumentu hodnotící studie, časopisecké články, práce podpořená grantem
PubMed
16288867
DOI
10.1016/j.bmcl.2005.10.059
PII: S0960-894X(05)01322-3
Knihovny.cz E-zdroje
- MeSH
- acetylcholinesterasa metabolismus MeSH
- bromované uhlovodíky chemická syntéza farmakologie MeSH
- cholinesterasové inhibitory farmakologie MeSH
- dursban farmakologie MeSH
- dusík chemie MeSH
- krysa rodu Rattus MeSH
- oximy chemie MeSH
- pyridinové sloučeniny chemická syntéza farmakologie MeSH
- reaktivátory cholinesterázy farmakologie MeSH
- vztah mezi dávkou a účinkem léčiva MeSH
- zvířata MeSH
- Check Tag
- krysa rodu Rattus MeSH
- zvířata MeSH
- Publikační typ
- časopisecké články MeSH
- hodnotící studie MeSH
- práce podpořená grantem MeSH
- Názvy látek
- (E)-1-(2-hydroxyiminomethylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide MeSH Prohlížeč
- acetylcholinesterasa MeSH
- bromované uhlovodíky MeSH
- cholinesterasové inhibitory MeSH
- dursban MeSH
- dusík MeSH
- oximy MeSH
- pyridinové sloučeniny MeSH
- reaktivátory cholinesterázy MeSH
Six potential AChE reactivators were synthesized using modification of currently known synthetic pathways. Their potency to reactivate AChE inhibited by insecticide chlorpyrifos was tested in vitro. According to the results, (E)-1-(2-hydroxyiminomethylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide seems to be the most potent AChE reactivator. The reactivation potency of these compounds depends on structural factors such as constitution of the linking chain between both pyridinium rings, position of the oxime moiety at the pyridinium ring and presence of quaternary nitrogens.
Citace poskytuje Crossref.org
Two step synthesis of a non-symmetric acetylcholinesterase reactivator