Design, synthesis and biological evaluation of 3-[4-(7-chloro-quinolin-4-yl)-piperazin-1-yl]-propionic acid hydrazones as antiprotozoal agents

• N-Acylhydrazones derived from 7-chloro-4-piperazin-1-yl-quinoline were synthesized.
• Potent and selective antimalarial and antiamoebic compounds were identified.
• N-Acylhydrazone (F12) inhibits the Plasmodium falciparum life cycle with good selectivity.
• N-Acylhydrazone (F12) inhibits the β-hematin formation.
• N-Acylhydrazone (F24) is an amoebicidal agent as potent as metronidazole.

N-Acylhydrazones derived from 7-chloro-4-piperazin-1-yl-quinoline were synthesized and biologically evaluated for blood-stage of Plasmodium falciparum and Entamoeba histolytica trophozoites. N-Acylhydrazone F12 was found to inhibit the P. falciparum growth as well as its life cycle with good selectivity, which was achieved by inhibiting hematin formation. Compound F24 showed better IC50 value than the amoebicidal drug metronidazole.

N-Acylhydrazones derived from 7-chloro-4-piperazin-1-yl-quinoline were synthesized and evaluated for blood-stage of Plasmodium falciparum, Entamoeba histolytica trophozoites, and cytotoxicity assay in mammalian cells.Figure optionsDownload as PowerPoint slide