DESIGN AND SYNTHESIS OF SOME ARYLHYDRAZONE DERIVATIVES AS POTENTIAL FAAH INHIBITORS

Abstract

Objective: The aim was to design, synthesis and investigation of possible interactions in the enzyme active site of a series of arylhydrazone derivatives for the inhibition of the FAAH enzyme. Material and Method: Arylhydrazone derivatives were obtained through the reaction of nicotinic hydrazide or benzohydrazide with appropriate aldehyde derivatives, and the obtained crude product was recrystallized from ethanol. After elucidating chemical structures of the compounds via spectroscopic methods, the inhibitory activities against hFAAH were screened. The results were further supported with molecular modeling studies. Result and Discussion: In this study, a new series of seven arylhydrazone derivatives were screened against hFAAH. 4-phenoxyphenyl bearing derivative 5 was found to inhibit hFAAH 40 % at 10 µM which indicates that newly developed inhibitor could serve as a starting point for improving inhibitory effect of the new series.