Design and synthesis of high affinity inhibitors of Plasmodium falciparum and Plasmodium vivax N-myristoyltransferases directed by ligand efficiency dependent …

…, JA Brannigan, K Rangachari, S Meister…

Index: Rackham, Mark D.; Brannigan, James A.; Rangachari, Kaveri; Meister, Stephan; Wilkinson, Anthony J.; Holder, Anthony A.; Leatherbarrow, Robin J.; Tate, Edward W. Journal of Medicinal Chemistry, 2014 , vol. 57, # 6 p. 2773 - 2788

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Citation Number: 29

Abstract

N-Myristoyltransferase (NMT) is an essential eukaryotic enzyme and an attractive drug target in parasitic infections such as malaria. We have previously reported that 2-(3-(piperidin-4- yloxy) benzo [b] thiophen-2-yl)-5-((1, 3, 5-trimethyl-1 H-pyrazol-4-yl) methyl)-1, 3, 4- oxadiazole (34c) is a high affinity inhibitor of both Plasmodium falciparum and P. vivax NMT and displays activity in vivo against a rodent malaria model. Here we describe the ...