Malaria is oldest and the most important tropical diseases known to mankind, for which chloroquine (CQ) has been the primary therapy of choice for past several decades. However, CQ-resistant Plasmodium falciparum is now observed in majority of the malaria-endemic regions, leading to the most deadly form of malaria. This warrants urgent need to develop more effective drugs against this parasite. Quinoxaline-based compounds display diverse biological activities as antibacterial, antiviral, anticancer and antiparasitic agents. In the present study we synthesized a small chemical library of new compounds based on quinoxaline and investigated their effect on the growth of M1 alanyl-aminopeptidase (PfAPN), an enzyme involved in the terminal stages of hemoglobin digestion to generate an amino acid pool within the parasite. Also, to check if these molecules affect parasite growth, the most lethal human malaria parasite P. falciparum was grown in the presence of varying concentration of these compounds, and IC50 concentrations for each compound were determined. We found these compounds cause enzyme inhibition, and also parasite growth inhibition with IC50 values in the low micromoles. Details of the study will be presented.

Study of quinoxaline-based new compounds against aminopeptidase N, and Plasmodium falciparum malarial parasite

247th National Meeting (2014)

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