Synthesis and antitrypanosomal activities of novel pyridylchalcones

Eur J Med Chem. 2017 Mar 10:128:213-218. doi: 10.1016/j.ejmech.2017.01.027. Epub 2017 Jan 23.

Abstract

A library of novel pyridylchalcones were synthesised and screened against Trypanosoma brucei rhodesiense. Eight were shown to have good activity with the most potent 8 having an IC50 value of 0.29 μM. Cytotoxicity testing with human KB cells showed a good selectivity profile for this compound with a selectivity index of 47. Little activity was seen when the library was tested against Leishmania donovani. In conclusion, pyridylchalcones are promising leads in the development of novel compounds for the treatment of human African trypanosomiasis (HAT).

Keywords: Claisen-Schmidt; Leishmania donovani; Neglected tropical disease; Pyridylchalcone; Trypanosoma brucei rhodesiense.

MeSH terms

  • Animals
  • Cells, Cultured
  • Chagas Disease / drug therapy*
  • Chagas Disease / parasitology
  • Chalcones / chemistry*
  • Humans
  • Leishmania donovani / drug effects
  • Leishmaniasis, Visceral / drug therapy
  • Leishmaniasis, Visceral / parasitology
  • Models, Molecular
  • Molecular Structure
  • Parasitic Sensitivity Tests
  • Propane / analogs & derivatives*
  • Propane / chemical synthesis
  • Propane / pharmacology
  • Pyridines / chemical synthesis*
  • Pyridines / pharmacology*
  • Structure-Activity Relationship
  • Trypanocidal Agents / chemical synthesis*
  • Trypanocidal Agents / pharmacology*
  • Trypanosoma cruzi / drug effects*

Substances

  • 1-(3-bromophenyl)-3-(3-pyridinyl)prop-2-en-1-one
  • Chalcones
  • Pyridines
  • Trypanocidal Agents
  • Propane