Design,synthesis and biological evaluation of quinazolin-4(3H)-one Schiff base conjugates as potential antiamoebic agents |
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| Authors: | Saba Tariq Fernando Avecilla Guru Prasad Sharma Neelima Mondal Amir Azam |
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| Affiliation: | 1. Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India;2. Departamento de Química Fundamental, Universidade da Coruña, Campus da Zapateira s/n, 15071 A Coruña, Spain;3. School of Life Sciences, Jawaharlal Nehru University, New Delhi 110062, India |
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| 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. |
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| Keywords: | Amebiasis MTT assay Antiamoebic activity 1,2,4-Triazole |
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