Discovery of Novel and Ligand-Efficient Inhibitors of Plasmodium falciparum and Plasmodium vivax N-Myristoyltransferase

作者：Rackham Mark D; Brannigan James A; Moss David K; Yu Zhiyong; Wilkinson Anthony J; Holder Anthony A; Tate Edward W; Leatherbarrow Robin J^*

来源：Journal of Medicinal Chemistry, 2013, 56(1): 371-375.

DOI：10.1021/jm301474t

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 (PO 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.

• 出版日期2013-1-10
• 单位河北医科大学