Discovery of Novel and Ligand-Efficient Inhibitors of Plasmodium falciparum and Plasmodium vivaxN-Myristoyltransferase

@inproceedings{Rackham2013DiscoveryON,
  title={Discovery of Novel and
Ligand-Efficient Inhibitors of Plasmodium falciparum and Plasmodium vivaxN-Myristoyltransferase},
  author={Mark D. Rackham and James A Brannigan and David K. Moss and Zhiyong Yu and Anthony James Wilkinson and Anthony A. Holder and Edward W Tate and Robin J. Leatherbarrow},
  booktitle={Journal of medicinal chemistry},
  year={2013}
}
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… CONTINUE READING