Detailed project information
| Title | : | Synthesis and biological evaluation of febrifugine derivatives as antimalarial agents |
| Applicant | : | Prof. dr. F.P.J.T. Rutjes |
| Research institute | : | Radboud Universiteit Nijmegen Subfaculteit Scheikunde Organische Chemie |
| Team members | : | Dr. C. Soares de Melo |
| Location | : | Radboud Universiteit Nijmegen |
| Duration | : | 12/01/2006 tot 05/18/2011 |
| Finance | : | Eur 55.000 |
| Subsidy | : | DC Fellowship (subsidy/programme has been discontinued and information is no longer available) |
Summary
Malaria is a worldwide life-threatening disease transmitted by parasites which are developing unacceptable levels of resistance to available drugs. The aim of this project is to synthesize new compounds with potential to display suitable antimalarial properties based on the lead compound febrifugine. This natural product was isolated as one of the active components from the roots of Dichroa febrifuga, a saxifragaceous plant, which has been employed in local Chinese traditional medicine for the treatment of malaria fevers for centuries with no reported parasite resistance.
The aim of this project can be subdivided in the following four objectives:
1. Development of new and flexible synthetic pathways to febrifugine
2. Synthesis of libraries of analogues, based on these pathways
3. Probing SAR data of the compounds for in vitro and in vivo antimalarial activity
4. Probing the mechanism of action of identified lead compounds
By following this approach, this project may eventually lead to new efficient drugs against malaria.
Products
Proefschriften
- Dr. C. Soares de Melo (2011). Synthesis and biological evaluation of febrifugine and derivatives as antimalarial agents. Radboud Universiteit Nijmegen. promotiedatum 5-12-2011. ISBN 9789461911070.
