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Discovery of Plasmodium vivax N-myristoyltransferase inhibitors: screening, synthesis, and structural characterization of their binding mode

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JournalJOURNAL OF MEDICINAL CHEMISTRY
DatePublished - 12 Apr 2012
Issue number7
Volume55
Number of pages5
Pages (from-to)3578-82
Original languageEnglish

Abstract

N-Myristoyltransferase (NMT) is a prospective drug target against parasitic protozoa. Herein we report the successful discovery of a series of Plasmodium vivax NMT inhibitors by high-throughput screening. A high-resolution crystal structure of the hit compound in complex with NMT was obtained, allowing understanding of its novel binding mode. A set of analogues was designed and tested to define the chemical groups relevant for activity and selectivity.

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