Metronidazole hydrazone conjugates: Design, synthesis, antiamoebic and molecular docking studies

[Display omitted] 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 sho...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2015-09, Vol.25 (17), p.3545-3549
Hauptverfasser: Ansari, Mohammad Fawad, Siddiqui, Shadab Miyan, Agarwal, Subhash M., Vikramdeo, Kunwar Somesh, Mondal, Neelima, Azam, Amir
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Sprache:eng
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Zusammenfassung:[Display omitted] 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 72h 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2015.06.091