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

Avecilla, Fernando; Tariq, Saba; Mondal, Neelima; Azam, Amir; Sharma, Guru Prasad

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http://hdl.handle.net/2183/38891

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

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Avecilla_Porto_Fernando_2018_Design_synthesis_and_biological_evaluation_of_quinazolin.pdf (1.83 MB)

Identifiers

URI: http://hdl.handle.net/2183/38891

DOI: 10.1016/J.JSCS.2016.05.006

Publication date

2018

Authors

Avecilla, Fernando

Tariq, Saba

Mondal, Neelima

Azam, Amir

Sharma, Guru Prasad

Bibliographic citation

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.