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

Eur J Med Chem. 2014 Mar 21:75:67-76. doi: 10.1016/j.ejmech.2014.01.023. Epub 2014 Jan 24.

Abstract

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.

Keywords: Acylhydrazone; Aminoquinoline; Amoebiasis; Malaria; Piperazinyl derivatives.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antiprotozoal Agents / chemistry*
  • Antiprotozoal Agents / pharmacology*
  • Drug Design
  • Entamoeba histolytica / drug effects*
  • Entamoebiasis / drug therapy
  • Humans
  • Hydrazones / chemistry*
  • Hydrazones / pharmacology*
  • Malaria, Falciparum / drug therapy
  • Plasmodium falciparum / drug effects*
  • Propionates / chemistry
  • Propionates / pharmacology

Substances

  • Antiprotozoal Agents
  • Hydrazones
  • Propionates
  • propionic acid