New readily accessible peroxides with high anti-malarial potency

Bioorg Med Chem Lett. 2002 Jan 7;12(1):69-72. doi: 10.1016/s0960-894x(01)00673-4.

Abstract

In an explorative study for new anti-malarial substances using the methyl esters (1 and 2) of peroxyplakoric acids A(3) and B(3) as scaffolds, 6-carbomethoxymethyl-3-methoxy-3-pentyl-1,2-dioxane, which has been readily synthesized from 6-keto-alpha,beta-unsaturated ester, was found to exhibit potent anti-malarial activity with high selective toxicity.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Antimalarials* / chemical synthesis
  • Antimalarials* / pharmacology
  • Dioxanes / chemical synthesis
  • Dioxanes / pharmacology
  • Drug Evaluation, Preclinical
  • Inhibitory Concentration 50
  • Peroxides / chemical synthesis
  • Peroxides / pharmacology*
  • Plasmodium falciparum / drug effects
  • Porifera / chemistry
  • Propionates / chemical synthesis
  • Propionates / pharmacology
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Antimalarials
  • Dioxanes
  • Peroxides
  • Propionates
  • plakoric acid