Design, synthesis and biological evaluation of quinazolin-4(3H)-one Schiff base conjugates as potential antiamoebic agents

Abstract In an effort to develop novel antiamoebic scaffolds having better efficacy than the standard drug metronidazole (IC 50  = 1.80 μM) used against Entamoeba histolytica , quinazolin-4(3 H )-one Schiff base conjugates were synthesized and evaluated against HM1: IMSS strain of E. histolytica . Out of the thirteen compounds ( S2 - S14 ), six compounds ( S2 , S3 , S4 , S5 , S6 and S11 ) were found to be better inhibitors than metronidazole and showed low cytotoxicity on HeLa cells, a cervical cancer cell line. The structure of intermediate compound S1 was confirmed by crystal structure studies.