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J Med Chem. 2012 Oct 25;55(20):8879-90. doi: 10.1021/jm301160h. Epub 2012 Oct 15.

Design and synthesis of inhibitors of Plasmodium falciparum N-myristoyltransferase, a promising target for antimalarial drug discovery.

Author information

1
Department of Chemistry, Imperial College London, London SW7 2AZ, UK.

Abstract

Design of inhibitors for N-myristoyltransferase (NMT), an enzyme responsible for protein trafficking in Plasmodium falciparum , the most lethal species of parasites that cause malaria, is described. Chemistry-driven optimization of compound 1 from a focused NMT inhibitor library led to the identification of two early lead compounds 4 and 25, which showed good enzyme and cellular potency and excellent selectivity over human NMT. These molecules provide a valuable starting point for further development.

PMID:
23035716
PMCID:
PMC3863768
DOI:
10.1021/jm301160h
[Indexed for MEDLINE]
Free PMC Article

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