gamma-Substituted bis(pivaloyloxymethyl)ester analogues of fosmidomycin and FR900098

Arch Pharm (Weinheim). 2007 Dec;340(12):661-6. doi: 10.1002/ardp.200700107.

Abstract

The synthesis and in-vitro antimalarial activity of gamma-substituted bis(pivaloyloxymethyl)ester analogues of the drug candidate fosmidomycin have been investigated. In contrast to the high antimalarial activity of alpha-aryl substituted fosmidomycin analogues like alpha-phenylfosmidomycin, gamma-substituted derivatives display only weak to moderate activity against the chloroquine-sensitive strain 3D7 of Plasmodium falciparum.

MeSH terms

  • Animals
  • Antimalarials / chemical synthesis*
  • Antimalarials / chemistry
  • Antimalarials / pharmacology*
  • Esters
  • Fosfomycin / analogs & derivatives*
  • Fosfomycin / chemical synthesis
  • Fosfomycin / chemistry
  • Fosfomycin / pharmacology
  • Humans
  • Parasitic Sensitivity Tests
  • Plasmodium falciparum / drug effects
  • Structure-Activity Relationship

Substances

  • Antimalarials
  • Esters
  • Fosfomycin
  • fosmidomycin
  • 3-(N-acetyl-N-hydroxy)aminopropylphosphonic acid