Synthesis and antimalarial activities of some furoxan sulfones and related furazans

Eur J Med Chem. 2005 Dec;40(12):1335-40. doi: 10.1016/j.ejmech.2005.05.001. Epub 2005 Jun 24.

Abstract

Furoxan derivatives bearing a sulfone moiety at position 3 or 4 were synthesized and tested for their antimalarial action on the chloroquine-sensitive D10 and the chloroquine-resistant W2 strains of Plasmodium falciparum. The furazan analogues were considered for comparison. The most active compounds were the products in which the -SO2R groups are at the 3-position of the furoxan system. These latter substances displayed an antimalarial activity in the microM range, possibly related in part to their ability to release NO.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimalarials / chemical synthesis*
  • Antimalarials / chemistry
  • Antimalarials / pharmacology*
  • Molecular Structure
  • Oxadiazoles / chemical synthesis*
  • Oxadiazoles / chemistry
  • Oxadiazoles / pharmacology*
  • Parasitic Sensitivity Tests
  • Plasmodium falciparum / drug effects
  • Structure-Activity Relationship

Substances

  • Antimalarials
  • Oxadiazoles
  • furoxans