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J Med Chem. 2013 Jan 10;56(1):371-5. doi: 10.1021/jm301474t. Epub 2012 Dec 17.

Discovery of novel and ligand-efficient inhibitors of Plasmodium falciparum and Plasmodium vivax N-myristoyltransferase.

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  • 1Department of Chemistry, Imperial College London, South Kensington Campus, London, SW7 2AZ, U.K.

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 (Pf) 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.

PMID:
23170970
[PubMed - indexed for MEDLINE]
PMCID:
PMC3601602
Free PMC Article
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