Plasmodium falciparum a is protozoan parasite that causes deathly cases of malaria in humans. There is a pressing need for the discovery of new antimalarial agents due to the rapid spread of multidrug-resistant strains of this organism. Methionine aminopeptidase (MetAP) carries out an important cotranslational N-terminal methionine excision of nascent proteins and was shown to be essential for the survival of many bacteria. Methionine aminopeptidase 2 (PfMetAP2) is essential for P. falciparum making it an attractive antimalarial drug target. This poster focuses on the synthesis of potential inhibitors of PfMetAP2, identification of lead compounds from the synthesized inhibitors and compounds from Malaria Box collection, and design of novel PfMetAP2 inhibitors using structural biology and molecular modeling. Up to date, the analogues of nitroxoline were identified as the most potent inhibitors against PfMetAP2 with IC50 ranging from 60 to 100 �M and growth inhibition IC50 between 0.99 to 3.74 �M respectively.

Inhibitors of plasmodium falciparum methionine aminopeptidase 2 with antimalarial activities

247th National Meeting (2014)

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