In vitro Reactivation of Chlorpyrifos-inhibited Rat Brain Acetylcholinesterase from 2-Quinolone Substituted Thiazole derivatives

摘要

Organophosphate (OP) compounds exert inhibition of acetylcholinesterase (AChE) by irreversibly binding to catalytic site of an enzyme. Despite continued efforts to discover improved reactivators, there has been little success towards innovation of AChE reactivators. In the present investigation, new series of 2-quinolone fused thiazole derivatives 3a-3f and 4a-4f were evaluated for their in vitro reactivation efficacy against chlorpyrifos inhibited AChE using 2-PAM as standard. Even though the non oxime derivatives were not as effective as pralidoxime (2-PAM), but exhibited considerable AChE reactivation. The compounds, 3b, 3c, 3f, and 4f, showed promising reactivation against chlorpyrifos inhibited AChE.