Synthesis of 2,4,6-trisubstituted pyrimidines as antimalarial agents

Bioorg Med Chem. 2005 Aug 1;13(15):4645-50. doi: 10.1016/j.bmc.2005.04.061.

Abstract

A series of 2,4,6-trisubstituted-pyrimidines were synthesized and evaluated for their in vitro antimalarial activity against Plasmodium falciparum. Of the 18 compounds synthesized, 14 compounds have shown MIC in the range of 0.25-2 microg/mL. These compounds are in vitro severalfold more active than pyrimethamine.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimalarials / chemical synthesis*
  • Antimalarials / chemistry
  • Antimalarials / pharmacology*
  • Molecular Structure
  • Plasmodium falciparum / drug effects*
  • Pyrimidines / chemical synthesis
  • Pyrimidines / chemistry*
  • Pyrimidines / pharmacology*
  • Structure-Activity Relationship

Substances

  • Antimalarials
  • Pyrimidines