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Interdisciplinarity in the rational design of enzyme inhibitory antimalarial drugs

Abstract:

The rational development of pharmaceutical agents is a laborious and demanding research field. Success in this chemical design depends on the integration of different areas of knowledge. In this context, interdisciplinarity is basic in the search for active and safety molecules based on structural and ontological knowledge of the therapeutic target. In this review we show the results of recent research on the rational design of antimalarial drugs supported on the structure of some enzymes of Plasmodium falciparum, particularly plasmepsin and falcipain, the main targets of the study-type enzyme inhibitors presented. We also consider the benefits and limitations of this kind of research. So far, the investigations have shown the potential of some chemical families such as those based on alofenilnorestatin, 1.4-benzodiazepine, vinyl sulfonamides, esters vinilsulfonates, 2H-isoquinolin-3-one, among some others, to inhibit hemoglobinases. These compounds are suitable to optimization by structural modifications in order to get more effective alternative compounds than the antiplasmodial agents available today.