Synthesis, characterization and antiamoebic activity of some hydrazone and azole derivatives bearing pyridyl moiety as a promising heterocyclic scaffold

In an effort to develop effective antiamoebic agents, some hydrazones and azoles containing pyridyl moiety were synthesized and screened for in vitro antiamoebic activity against HM1:IMSS strain of Entamoeba histolytica. Among all the compounds, only five compounds (1, 3, 5, 9 and 11) were found to be better inhibitors of growth of E. histolytica than the reference drug metronidazole. The cytotoxic studies of these compounds on human breast cancer MCF-7 cell line revealed that all the compounds were low-cytotoxic in the concentration range of 2.5–250 μM.

Hydrazone and azole derivatives bearing pyridyl moiety were synthesized and found better inhibitors of Entamoeba histolytica than the standard drug metronidazole.Figure optionsDownload as PowerPoint slideHighlights
► Hydrazone and azole derivatives bearing pyridyl moiety were synthesized.
► All the compounds were evaluated for antiamoebic activities.
► Five compounds were found more active than the reference drug metronidazole.
► Five compounds were non-cytotoxic against the human breast cancer MCF-7 cell line.