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In vitro and mouse studies have identified a new class of antiparasitic compounds that could help treat malaria. Chemical synthesis and in vitro testing of amino benzimidazole analogs identified several compounds that inhibited growth of the asexual blood stage of Plasmodium falciparum, including drug-resistant strains, at nanomolar IC50 values without causing cytotoxicity in a mammalian cell line. In a humanized mouse model of malaria, a lead member of the series decreased parasitemia in a dose-dependent manner with potency comparable to that of the generic antimalarial drug chloroquine. Next steps could include optimizing and testing the compounds against drug-resistant strains of P. falciparum.

SciBX 7(28); doi:10.1038/scibx.2014.829
Published online July 24, 2014

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Hameed P, S. et al. J. Med. Chem.; published online June 10, 2014;
Contact: Sreekanth Ramachandran, AstraZeneca India Pvt. Ltd., Bangalore, India
Contact: Vasan Sambandamurthy, same affiliation as above