Discovery of a Novel Class of Orally Active Trypanocidal N-Myristoyltransferase Inhibitors

Abstract

N-Myristoyltransferase (NMT) represents a promising drug target for human African trypanosomiasis (HAT), which is caused by the parasitic protozoa Trypanosoma brucei. We report the optimization of a high throughput screening hit (1) to give a lead molecule DDD85646 (63), which has potent activity against the enzyme (IC(50) = 2 nM) and T. brucei (EC(50) = 2… (More)
DOI: 10.1021/jm201091t

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