Anti-infective drugs & redox chemistry
A research applied to medicinal chemistry and, in particular, to the synthesis and investigation of inhibitors of NADPH-dependent oxido-reductases is conducted with the aim to develop original antiinfectious agents (e.g. menadione series) and to identify new targets for antiparasitic chemotherapy. Our interdisciplinary activity spans from the synthesis (inhibitors, redox-active compounds, fluorescent tools, photoaffinity labels of targeted proteins) to enzymology and understanding of the mechanisms of action in situ in living parasites. Among our recent major achievements, we showed that potent antiparasitic drug-candidates, displaying a 3-benzyl-menadione scaffold, induce distinct phenotypic effects in parasites according to their substitution patterns. Our research efforts are now focused on the optimization of our antimalarial lead compound, i.e. plasmodione, a fast acting and transmission blocking agent, and on the development of chemical tools for metabol- and proteo-omics via a click & fish strategy.
- (Bio)(in)organic chemistry & fluorescent tools
Unraveling the mechanisms of action is also guided by physico-chemical approaches under quasi-physiological conditions to describe the interactions of antiinfectious agents with relevant biotargets. Structure-activity relationships are harmoniously synergized to chemoinformatics (local collaboration) to optimize the drug design. Efforts are also directed to the development of ratiometric fluorescent probes for local pH or redox measurements in living parasites.
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