SYNTHESIS OF UDP-GALACTOFURANOSE ANALOGS AS MECHANISTIC PROBES OF UDP_GALACTOPYRANOSE MUTASE
In the fight against Multi-drugs resistant strains ofMycobacterium tuberculosis[1], novel therapeutic targets such as UDP-Galactopyranose Mutase (UGM) have been identified. This enzyme, absent in mammals, interconverts UDP-Galactopyranose1into UDP-Galactofuranose3. UDP-galf3is the activated precursor of galactofuranose residuesthat are essential components of the cell wall biosynthesis of major pathogens such asK. Pneumoniae,M. Tuberculosis,L. majorandT. cruzi.
In order to probe the UGM binding pocket, we synthesized different potential inhibitors, such as C-glycosidic analogues of UDP-Gal (conformational probes),[2a]exo-glycals[2b-d]and some acyclic galactose derivatives[3]. Here we report the synthesis and the inhibition evaluation of these inhibitors against UGM.
References
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