Email

serge.vancalenbergh@ugent.be

Telephone

+32 9 264 8124

Fax

+32 9 264 8146

Institution

University of Ghent (Ghent)

Address

Faculteit Farmaceutische Wetenschappen / Laboratory for Medical Chemistry
Harelbekestraat 72
BE-9000

Ghent

Belgium

Home Page

http://www.ugent.be

Serge Van Calenbergh

The central interest of our research group (currently comprising 6 PhD students and 2 postdocs) is structure-based drug design and synthesis of small molecules with pharmacological relevance (with particular interest in neglected diseases like TB and malaria). From a chemical point of view we are mainly engaged in the synthesis of nucleoside and sphingolipid analogues.

Recently, we started a collaboration with the group of Dr. Hassan Jomaa aiming at designing inhibitors for several targets of the non-mevalonate pathway.

It is well established that fosmidomycin, an antibacterial phosphonate, demonstrates potent antimalarial activity by inhibiting 1-deoxy-D-xylulose-5-phosphate reductoisomerase (DXR), the second enzyme involved in this pathway. By substituting or altering the three carbon spacer of fosmidomycin, we designed several analogues of this valuable lead. Introduction of an 3,4-dichlorophenyl group in the a -position of the phosphonic acid, for instance, yielded an analogue that proved significantly more potent than fosmidomycin in inhibiting Dd2 and 3D7 P. falciparum strains.