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Discovery of Novel and Ligand-Efficient Inhibitors of Plasmodium falciparum and Plasmodium vivax N-Myristoyltransferase

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JournalJOURNAL OF MEDICINAL CHEMISTRY
DateE-pub ahead of print - 22 Nov 2012
DatePublished (current) - 10 Jan 2013
Issue number1
Volume56
Number of pages5
Pages (from-to)371-375
Early online date22/11/12
Original languageEnglish

Abstract

N-Myristoyltransferase (NMT) is an attractive antiprotozoan drug target. A lead-hopping approach was utilized in the design and synthesis of novel benzo[b]thiophene-containing inhibitors of Plasmodium falciparum (PO and Plasmodium vivax (Pv) NMT. These inhibitors are selective against Homo sapiens NMT1 (HsNMT), have excellent ligand efficiency (LE), and display antiparasitic activity in vitro. The binding mode of this series was determined by crystallography and shows a novel binding mode for the benzothiophene ring.

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