Design, synthesis and biological evaluation of quinazolin-4(3H)-one Schiff base conjugates as potential antiamoebic agents
Journal of Saudi Chemical Society(2018)
摘要
In an effort to develop novel antiamoebic scaffolds having better efficacy than the standard drug metronidazole (IC50=1.80μM) used against Entamoeba histolytica, quinazolin-4(3H)-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.
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关键词
Amebiasis,MTT assay,Antiamoebic activity,1,2,4-Triazole
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