Metronidazole hydrazone conjugates: Design, synthesis, antiamoebic and molecular docking studies
Mohammad Fawad Ansari1, Shadab Miyan Siddiqui1, Subhash M Agarwal2
1Department of Chemistry, Jamia Millia Islamia, Jamia Nagar, New Delhi 110025, India.
Abstract:
Metronidazole hydrazone conjugates (2-13) were synthesized and screened in vitro for antiamoebic activity against HM1: IMSS strain of Entamoeba histolytica. Six compounds were found to be better inhibitors of E. histolytica than the reference drug metronidazole. These compounds showed greater than 50-60% viability against HeLa cervical cancer cell line after 72 h treatment. Also, molecular docking study was undertaken on E. histolytica thioredoxin reductase (EhTHRase) protein which showed significant binding affinity in the active site. Out of the six actives, some of the compounds showed lipophilic characteristics.
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