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European Pharmaceutical Students’ Association
SYNTHESIS AND CHARACTERIZATION OF CHLOROQUINE CLICK DERIVATIVES WITH POTENTIAL ANTIMALARIAL ACTIVITY Author: Marko Dužević Scientific Coordinator: doc. dr. sc. Ivana Perković Institution: Faculty of Pharmacy and Biochemistry at University of Zagreb
Malaria is one of the most prevalent parasitic diseases in the world, ranked by the WHO in 2016 as the 6th most common cause of death in low-developed countries. Although positive progress has been made in its treatment and prevention over the past decade, there is still a great need for the development of new antimalarials due to the emergence and spread of strains resistant to conventional drugs. Until the advent of newer molecules, in the past, due to its good safety profile, efficacy, and cost-effective synthesis, chloroquine was used very often and is still used today as a model drug for the development of new alternative antimalarials. To enhance its antiplasmodial activity on resistant strains, four new quinoline-1H-1,2,3-triazole hybrids with harmine, an alkaloid of plant origin that also has antimalarial activity, were synthesized using method of copper-catalysed azide–alkyne cycloaddition. The reactions of organic azides and alkynes catalysed by copper species represent the prototypical examples of click chemistry. This paper presents the procedures for their synthesis and the results of structural characterization by analytical and spectroscopic techniques. All synthesized compounds have shown the potential for good oral bioavailability, and further research, which goes beyond the scope of this paper, will examine their antiparasitic effects on species of the genus Plasmodium.
Newly synthesised molecules presented in the paper
