Design, synthesis and biological evaluation of quinazolin-4(3H)-one Schiff base conjugates as potential antiamoebic agents
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Design, synthesis and biological evaluation of quinazolin-4(3H)-one Schiff base conjugates as potential antiamoebic agentsDate
2018Citation
Tariq, S., Avecilla, F., Sharma, G. P., Mondal, N., & Azam, A. (2018). Design, synthesis and biological evaluation of quinazolin-4(3H)-one Schiff base conjugates as potential antiamoebic agents. Journal of Saudi Chemical Society, 22(3), 306-315. https://doi.org/10.1016/J.JSCS.2016.05.006
Abstract
[Abstract] In an effort to develop novel antiamoebic scaffolds having better efficacy than the standard drug metronidazole (IC50 = 1.80 μM) 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.
Keywords
Amebiasis
MTT assay
Antiamoebic activity
1,2,4-Triazole
MTT assay
Antiamoebic activity
1,2,4-Triazole
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CC BY-NC-ND 4.0 Attribution-NonCommercial-NoDerivatives 4.0 International