Chalcone hybrids as privileged scaffolds in antimalarial drug discovery: A key review

Eur J Med Chem. 2020 May 1:193:112215. doi: 10.1016/j.ejmech.2020.112215. Epub 2020 Mar 9.

Abstract

Malaria remains a serious worldwide health danger and massive economic trouble to disease-endemic nations. Presently, 250 million of malarial cases are expected worldwide. The emergence of fighting of the Plasmodium parasite against the first-line antimalarial drugs has fueled research attention in the way of designing new scaffolds as well as strategies to counter the drug resistance. Chalcones are simple and well-known analogs, which were found in a huge number of natural compounds and also been prepared according to their suitable synthetic approaches. This review illustrates the current progresses on structure-activity relationship (SAR) and mechanism of diverse types of chalcone derivatives that play a significant role for the development of novel safe, less toxic and highly active antimalarials. This present mini-review will be useful to scientists in research fields of medicinal chemistry, organic synthesis, and also various biological applications particularly for the development of novel antiplasmodial and antimalarial agents.

Keywords: Antimalarial; Antiplasmodial; Chalcone; Structure-activity relationships.

Publication types

  • Review

MeSH terms

  • Animals
  • Antimalarials / chemical synthesis
  • Antimalarials / chemistry
  • Antimalarials / pharmacology*
  • Chalcone / chemical synthesis
  • Chalcone / chemistry
  • Chalcone / pharmacology*
  • Dose-Response Relationship, Drug
  • Drug Discovery*
  • Humans
  • Malaria / drug therapy*
  • Molecular Structure
  • Parasitic Sensitivity Tests
  • Plasmodium falciparum / drug effects*
  • Structure-Activity Relationship

Substances

  • Antimalarials
  • Chalcone