Synthesis, characterization, antiamoebic activity and cytotoxicity of novel series of pyrazoline derivatives bearing quinoline tail

The cyclization of chalcones (1a–1j) with 2-(quinolin-8-yloxy) acetohydrazide (2) under basic condition led to the formation of new compounds, pyrazoline derivatives (3a–3j). In vitro antiamoebic activity was performed against HM1: IMSS strain of Entamoeba histolytica. The results showed that the compounds 3d, 3g, 3h, and 3j exhibited promising antiamoebic activity (IC50 = 0.05 μM, 0.31 μM, 0.06 μM, 0.29 μM) respectively than the standard drug metronidazole (IC50 = 1.84 μM). The toxicological studies of these compounds on human breast cancer MCF-7 cell line showed that all the compounds 3d, 3g, 3h, 3j and metronidazole were nontoxic at the concentration range of 1.56–50 μM.

Graphical abstractNovel pyrazoline derivatives (3a–3j) were synthesized. Compounds 3d, 3g, 3h and 3j exhibited better antiamoebic activity and screened for toxicity.Figure optionsDownload full-size imageDownload as PowerPoint slide