Synthesis and investigation of activities and modes of action of antimalarial compounds

© 2015 Dr. Silvia Carolina TeguhSyntheses, structure-activity relationships and mode of action investigations of a novel compound series of conjugated quinoline-indole, revealed that they are active against blood stages of multiple strains of Plasmodium falciparum, and appear to dissipate mitochondrial potential. To aid in the study of current antimalarial drug, artemisinin, components of a “bait-and-probe” strategy were synthesised (using click chemistry). The work in this thesis has shown that the azide-linked drug-“bait” can be covalently incorporated into a protein, which acts as a potential drug target, prior to being coupled with its identifier “probe” (e.g. biotin)