<i>Plasmodium falciparum</i> is the species responsible for 85% of the malaria cases. Malaria is endemic to over 100 nations and territories in Africa, Asia, Latin America, the Middle East, and the South Pacific and rising rates of drug resistance make finding novel drugs imperative. Towards this end, we have investigated aminomethylphenols with the aims of improving anti-plasmodium potency and metabolic stability. Aminomethylphenol analog synthesis focused on substituting different groups off the aminomethyl position. Structure activity relationship (SAR) analysis of the analogs revealed anti-plasmodium 3D7 IC50 values as low as 120 nM. 3D7 potency SAR and metabolic stability in mouse liver microsomes will be presented, illustrating the potential for greater metabolic stability and anti-plasmodium potency in this series.

Synthesis and evaluation of aminomethylphenols as anti-malarial agents

251st National Meeting (2016)

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