Article
Design and synthesis of inhibitors of Plasmodium falciparum N-myristoyltransferase, a promising target for antimalarial drug discovery.
Journal of medicinal chemistry - 25 Oct 2012
Yu Zhiyong, Brannigan James A, Moss David K, Brzozowski A Marek, Wilkinson Anthony J, Holder Anthony A, Tate Edward W, Leatherbarrow Robin J
Abstract excerpt
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...
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