A comprehensive review of chalcone derivatives as antileishmanial agents

Eur J Med Chem. 2018 Apr 25:150:920-929. doi: 10.1016/j.ejmech.2018.03.047. Epub 2018 Mar 22.

Abstract

Leishmaniasis is a group of infectious neglected tropical diseases caused by more than 20 pathogenic species of Leishmania sp. Due to the limitations of the current treatments available, chalcone moiety has been drawn with a lot of attention due to the simple chemistry and synthesis, being reported with antileishmanial activity in particular against amastigote form. This review aims to provide an overview towards antileishmanial activity of chalcones derivatives against amastigote form for Leishmania major, L. amazonensis, L. panamensis, L. donovani and L. infantum as well as their structure-activity relationship (SAR), molecular targets and in silico ADMET evaluation. In this way, it is expected that this review may support the research and development of new promising chalcones candidates a leishmanicidal drugs.

Keywords: ADMET; Drug design; Leishmania; SAR.

Publication types

  • Review

MeSH terms

  • Antiprotozoal Agents / chemical synthesis
  • Antiprotozoal Agents / chemistry
  • Antiprotozoal Agents / pharmacology*
  • Chalcone / chemical synthesis
  • Chalcone / chemistry
  • Chalcone / pharmacology*
  • Dose-Response Relationship, Drug
  • Drug Design
  • Humans
  • Leishmania / drug effects*
  • Molecular Structure
  • Parasitic Sensitivity Tests
  • Structure-Activity Relationship

Substances

  • Antiprotozoal Agents
  • Chalcone