Synthesis and biological evaluation of 4-(2-(dimethylamino)ethoxy)benzohydrazide derivatives as inhibitors of Entamoeba histolyica

Eur J Med Chem. 2016 Nov 29:124:445-455. doi: 10.1016/j.ejmech.2016.08.022. Epub 2016 Aug 13.

Abstract

In the quest for potent antiamoebic agents, a series of hydrazone hybrids (H1H30) have been designed and sequentially synthesized. The dimethylaminoethoxy and hydrazone entities incorporated into one molecule proved to be more persuasive and selective approach towards designing of antiamoebic agent. The synthesized compounds exhibited promising results against E. histolytica. The compound N'-(2-chlorobenzylidene)-4-(2-(dimethylamino) ethoxy)benzohydrazide was most impending among the series. Cytotoxicity profile showed better cell viability on lung cancer cell line (A549 cells) by MTT assay.

Keywords: Antiamoebic activity; Cytotoxicity; Hydrazones; MTT assay; X-ray crystallography.

MeSH terms

  • Antiprotozoal Agents / chemical synthesis*
  • Antiprotozoal Agents / chemistry
  • Antiprotozoal Agents / pharmacology*
  • Antiprotozoal Agents / toxicity
  • Cell Line, Tumor
  • Chemistry Techniques, Synthetic
  • Drug Evaluation, Preclinical
  • Entamoeba histolytica / drug effects*
  • Humans
  • Hydrazines / chemical synthesis*
  • Hydrazines / chemistry
  • Hydrazines / pharmacology*
  • Hydrazines / toxicity
  • Structure-Activity Relationship

Substances

  • Antiprotozoal Agents
  • Hydrazines