Project

Synthetic optimization of fosmidomycin (analogues) towards selection of a preclinical candidate that combines promising pharmacodynamic bioacailability properties.

Duration
01 March 2013 → 30 September 2016
Funding
Regional and community funding: Special Research Fund
Research disciplines
  • Natural sciences
    • Plant biology
  • 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
  • Agricultural and food sciences
    • Agricultural plant production
    • Horticultural production
Keywords
DOXP reductoiomerase malaria non-mevalonate pathway
 
Project description

A mevalonate independent pathway for isoprenoid biosynthesis the socalled MEP pahtway, has been discovered recentyly and validated as new drug targetfor with this pathway through inhibtion of DOXP reductoisomerase, is a promising clinicallly effective antimalarial agent. tHIS PROJECT AIMS AT THEFURTHER OPTIMIZATION OF THIS PROMISING LEAD VIA/

1)the synthesis of a series of novel ss-substituted fosmidocycin analogues.

2) the synthesis ofa small liberary of phosphoramidate prodrugs of fosmidoycin and analogues. Careful screening of the final compounds will be performed in colleboration with esteemed national and international research groups.