Structure-activity relationships in reactivators of organophosphorus-inhibited acetylcholinesterase. 9. N-Heterocyclic acraldoximes methiodides.
N-Heterocyclic acraldoximes methiodides, where the heterocyclic residues are 2-, 3-, and 4-pyridyl, 2-(1-methyl)imidazolyl or 4-pyrimidyl, were prepared and tested for their reactivating potency on acetylcholinesterase inhibited from diisopropylphosphorofluoridate (DFP). The in vitro testing revealed that the new compounds are good reactivators of the phosphorylated electric eel cholinesterase. The structure-activity relationships are briefly discussed.
D000171:Acrolein / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000494:pharmacology; D000447:Aldehydes / Q000138:chemical synthesis*; D000818:Animals; D002800:Cholinesterase Inhibitors; D002801:Cholinesterase Reactivators / Q000138:chemical synthesis*; D004593:Electrophorus / Q000378:metabolism; D007531:Isoflurophate / Q000037:antagonists & inhibitors; D009682:Magnetic Resonance Spectroscopy; D010091:Oximes / Q000138:chemical synthesis* / Q000494:pharmacology; D000644:Quaternary Ammonium Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D013056:Spectrophotometry, Ultraviolet
D000447:Aldehydes; D002800:Cholinesterase Inhibitors; D002801:Cholinesterase Reactivators; D010091:Oximes; D000644:Quaternary Ammonium Compounds; D007531:Isoflurophate; D000171:Acrolein