The Design, Synthesis and Evaluation of Novel Metalloaminopeptidase Inhibitors
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Approximately 247 million infections and 619,000 deaths associated with malaria were recorded in 2021. Malaria caused by Plasmodium falciparum has two enzymes, PfA-M1 and PfA-M17, which play vital roles in the fitness and survival of malaria parasites. Inhibition of PfA-M1 and PfA-M17 results in parasite death. Using the structures of PfA-M1 and PfA-M17, a range of new inhibitors were designed, synthesised, and evaluated for use as potential antimalarial agents. Several of these new compounds were found to be potent inhibitors of PfA-M1 and inhibited malaria parasites, with this work paving the way towards a new class of antimalarial therapy.
创建时间：
2023-04-13
