Discovery of novel 1H-imidazol-2-yl-pyrimidine-4,6-diamines as potential antimalarials

Bioorg Med Chem Lett. 2010 Jul 15;20(14):4027-31. doi: 10.1016/j.bmcl.2010.05.095. Epub 2010 Jun 2.

Abstract

A novel family of 1H-imidazol-2-yl-pyrimidine-4,6-diamines has been identified with potent activity against the erythrocyte-stage of Plasmodium falciparum (Pf), the most common causative agent of malaria. A systematic SAR study resulted in the identification of compound 40 which exhibits good potency against both wild-type and drug resistant parasites and exhibits good in vivo pharmacokinetic properties.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimalarials / chemistry*
  • Antimalarials / pharmacokinetics
  • Antimalarials / pharmacology
  • Drug Discovery
  • Plasmodium falciparum / drug effects*
  • Pyrimidines / chemistry*
  • Pyrimidines / pharmacokinetics
  • Pyrimidines / pharmacology
  • Structure-Activity Relationship

Substances

  • Antimalarials
  • Pyrimidines