Charged pyridinium oximes with thiocarboxamide moiety are equally or less effective reactivators of organophosphate-inhibited cholinesterases compared to analogous carboxamides.
Acetylcholinesterase
/ metabolism
Butyrylcholinesterase
/ metabolism
Cholinesterase Inhibitors
/ chemical synthesis
Dose-Response Relationship, Drug
Humans
Molecular Structure
Organophosphates
/ chemical synthesis
Oximes
/ chemical synthesis
Pyridinium Compounds
/ chemical synthesis
Structure-Activity Relationship
Sulfhydryl Compounds
/ chemical synthesis
Cholinesterase
inhibition
organophosphate
oxime
reactivation
Journal
Journal of enzyme inhibition and medicinal chemistry
ISSN: 1475-6374
Titre abrégé: J Enzyme Inhib Med Chem
Pays: England
ID NLM: 101150203
Informations de publication
Date de publication:
Dec 2022
Dec 2022
Historique:
entrez:
23
2
2022
pubmed:
24
2
2022
medline:
22
3
2022
Statut:
ppublish
Résumé
The organophosphorus antidotes, so-called oximes, are able to restore the enzymatic function of acetylcholinesterase (AChE) or butyrylcholinesterase (BChE) via cleavage of organophosphate from the active site of the phosphylated enzyme. In this work, the charged pyridinium oximes containing thiocarboxamide moiety were designed, prepared and tested. Their stability and p
Identifiants
pubmed: 35193448
doi: 10.1080/14756366.2022.2041628
pmc: PMC8881075
doi:
Substances chimiques
Cholinesterase Inhibitors
0
Organophosphates
0
Oximes
0
Pyridinium Compounds
0
Sulfhydryl Compounds
0
Acetylcholinesterase
EC 3.1.1.7
Butyrylcholinesterase
EC 3.1.1.8
Types de publication
Journal Article
Langues
eng
Sous-ensembles de citation
IM
Pagination
760-767Références
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