Novel antileishmanial chalconoids: synthesis and biological activity of 1- or 3-(6-chloro-2H-chromen-3-yl)propen-1-ones

Eur J Med Chem. 2010 Apr;45(4):1424-9. doi: 10.1016/j.ejmech.2009.12.046. Epub 2009 Dec 28.

Abstract

A series of novel chalconoids containing a 6-chloro-2H-chromen-3-yl group were prepared through a convenient and efficient synthetic method by using 5-chloro-2-hydroxybenzaldehyde as starting material. The target compounds were evaluated against the promastigote form of Leishmania major using MTT assay. All of the evaluated compounds have shown high in vitro antileishmanial activity at concentrations less than 3.0 microM. The results of cytotoxicity assessment against mouse peritoneal macrophage cells showed that these compounds display antileishmanial activity at non-cytotoxic concentrations.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antiprotozoal Agents / chemical synthesis*
  • Antiprotozoal Agents / chemistry
  • Antiprotozoal Agents / pharmacology*
  • Cells, Cultured
  • Chalcones / chemical synthesis*
  • Chalcones / chemistry
  • Chalcones / pharmacology*
  • Leishmania major / drug effects*
  • Macrophages, Peritoneal / drug effects
  • Magnetic Resonance Spectroscopy
  • Mass Spectrometry
  • Mice
  • Spectrophotometry, Infrared

Substances

  • Antiprotozoal Agents
  • Chalcones