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The Thai Journal of Pharmaceutical Sciences

Abstract

The present communication focused on synthesis, characterization and in vitro reactivation of chlorpyrifos inhibited acetylcholinesterase by pyrazole-oxime derivatives. A series of (E)-1-(phenyl)-3-(4-(dimethylamino)phenyl)prop-2-en-1-ones (1a-e) were synthesized from substituted acetophenone and aldehydes by adopting standard procedure. The intermediates 1-(5-(Phenyl)-3-(4-(dimethylamino)phenyl)-4,5-dihydropyrazol-1-yl)ethanones (2a-e) were synthesized by treating 1a-e with hydrazine hydrate in glacial acetic acid under the reflux. The title compounds (3a-e) were prepared by the condensation of (2a-e) with hydroxylamine hydrochloride in ethanol and pyridine as a base. The structures of all the newly synthesized products were confirmed by physicochemical and spectral analysis. All the synthesized compounds (3a-e) were screened for their intoxification of chlorpyrifos inhibited rat brain AChE by Ellman’s method. The data reveal that all the newly developed reactivators were not able to reactivate chlorpyrifos-inhibited AChE. Only two compounds of pyrazole oxime, 3a (35.2%, 60 min) and 3d (37.2%, 60 min) were found to be moderate reactivators as compared to standard (67.2%, 60 min).

DOI

10.56808/3027-7922.2789

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