Curcumin-related hybrid compounds as potential antimalarial agents : design, synthesis, mechanistic investigations, biological evaluation and pharmacokinetic studies
Doctoral Thesis
2010
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University of Cape Town
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Abstract
Malaria remains one of the most devastating tropical diseases, with staggering infection and mortality statistics. Over 200 million clinical cases of malaria (resulting in 1 - 3 million deaths) are reported annually. Africa bears the greatest burden of this disease. with the vast majority of malaria cases (>85%). and malaria-related deaths (>90%). being reported in sub-Saharan Africa. The main challenge to malaria control has been the development of clinically significant resistance Of the parasite to most known antimalarial drugs. This suggests that the development of new, highly efficadous drugs and/or treatment regimens for the management of malaria remains a key priority. This study applied molecular hybridization as a strategy in the development of novel potential antimalarial agents. The aim was to try and identify novel hybrid compounds containing scaffolds that are structurally related to the natural product curcumin, and which exhibit in vitro and in vivo antimalarial activity. Part of the study involved investigations into the pharmacokinetics and possible antimalarial mechanisms of action of selected target compounds.
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Includes bibliographical references.
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Guantai, E. 2010. Curcumin-related hybrid compounds as potential antimalarial agents : design, synthesis, mechanistic investigations, biological evaluation and pharmacokinetic studies. University of Cape Town.