National Center for
4B11: Plasmodium Vivax N-Myristoyltransferase With A Bound Benzofuran Inhibitor (Compound 13)
Design and Synthesis of Inhibitors of Plasmodium falciparum N-Myristoyltransferase, A Promising Target for Antimalarial Drug Discovery
J. Med. Chem. (2012) 55 p.8879-8890
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.
* Click molecule labels to explore molecular sequence information.