Collect. Czech. Chem. Commun. 1998, 63, 199-204

Cholinesterase Reactivators Derived from Pyridine-2-carbaldoxime

Jiří Bielavskýa, Jiří Kassaa, Iva Elsnerováa and Luboš Dejmekb

a J. E. Purkyně Military Medical Academy, 500 01 Hradec Králové, Czech Republic
b Research Institute for Pharmacy and Biochemistry, 130 60 Prague 3, Czech Republic


Monoquaternary reactivators of cholinesterase 3a-3c were prepared by quaternization of substituted pyridine-2-carbaldoximes with an ester (1a, 1b) or carbamoyl (2) function in position 4. A new bisquaternary reactivator, 4-carbamoyl-2'-[(hydroxyimino)methyl]-1,1'-(but-2-ene-1,4-diyl)bispyridinium salt (5), was derived from the unsubstituted pyridine-2-carbaldoxime. The compounds were characterized by UV spectra and ionization constants. The substances exhibit antidote effects in intoxications with organophosphate cholinesterase inhibitors.

Keywords: Reactivators; Cholinesterase; Pyridines; Pyridinium salts; Organophosphates.