Project

Development of alpha-subsituted fosmidomycin analogues as antimalarial DOXP reductoisomerase inhibitors

Duration
01 January 2007 → 30 December 2012
Funding
Research Foundation - Flanders (FWO)
Research disciplines
  • Natural sciences
    • Organic chemistry
  • Medical and health sciences
    • Biomarker discovery and evaluation
    • Drug discovery and development
    • Medicinal products
    • Pharmaceutics
    • Pharmacognosy and phytochemistry
    • Pharmacology
    • Pharmacotherapy
    • Toxicology and toxinology
    • Other pharmaceutical sciences
Keywords
malaria 2C-methyl-D-erythritol 4-phophate pathway DOXP reductoiomerase
 
Project description

A mevalonate independent pathway for isoprenoid biosynthesis, the so-called DOXP pathway, has been discovered recently and validated as new drug target. Fosmidomycin, a phosphonate that interferes with this pathway through inhibition of DOXP reductiosomerase, represents a promising antimalarial agent. This project aims at the development of alpha-substituted fosmidomycin analogues that are in vitro superior to fosmidomycin in inhibiting the growth of P. falciparum and other pathogens that use the non-mevalonate pathway.