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

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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Rackham MD,Brannigan JA,Moss DK,Yu Z,Wilkinson AJ,Holder AA,Tate EW,Leatherbarrow RJ

doi

10.1021/jm301474t

subject

Has Abstract

pub_date

2013-01-10 00:00:00

pages

371-5

issue

1

eissn

0022-2623

issn

1520-4804

journal_volume

56

pub_type

杂志文章

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