Synthesis of aminomethylthiazole analogues for evaluation as antiplasmodial agents
The World Health Organisation has estimated that about 219 million cases of malaria occurred in 2010 with an estimated 660,000 fatalities resulting. The disease is caused by five species of protozoan parasites of the genus Plasmodium with Plasmodium falciparum being the most virulent. Among the many shortfalls of current antimalarial drugs, the emergence of drug resistant strains of the malaria parasites is the most disturbing. Thus, there is an urgent need to develop new chemotherapeutic agents which can potentially target drug resistant strains of these parasites. Undertaking structure activity relationship (SAR) studies around biologically active compounds is one strategy that can identify analogues with superior activity and/or novel modes of action to circumvent drug resistance. In this dissertation, the synthesis, characterisation, and antiplasmodial evaluation of aminomethylthiazoles and related analogues are reported.
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