The application of the Multi-Component Reaction (MCR) strategy in the design and synthesis of new antiplasmodial and antimycobacterial agents
Doctoral Thesis
2012
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University of Cape Town
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Malaria and tuberculosis are ancient diseases that continue to have a profound impact on mankind, 5 millennia after their first documentation. Malaria is endemic in more than 100 countries and about 50% of the world's population is at risk of infection. Sub-Saharan Africa accounts for nearly 91% of malaria-related deaths annually. Tuberculosis on the other hand infects about one third of the word's population and is the second major cause of death in adults worldwide, with about 1.8 million deaths reported annually. The major challenge to the control of these diseases has been the rapid emergence of multi-drug resistant strains to the currently administered drugs, as such, these exert an enormous pressure on health care systems, especially in resource-limited areas. Alleviation of this pressure requires the development of highly efficacious new chemical entities (NCEs) to curb or manage these pathogens. The main aim of this study was to design NCEs based on quinoline-, PA-824-, and tetrazole-scaffolds, which exhibit in vitro antiplasmodial and antimycobacterial activity.
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Tukulula, M. 2012. The application of the Multi-Component Reaction (MCR) strategy in the design and synthesis of new antiplasmodial and antimycobacterial agents. University of Cape Town.