Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors

Tracy Bayliss, David Robinson, Victoria Smith, Stephen Brand, Stuart McElroy, Leah Torrie, Chidochangu Mpamhanga, Suzanne Norval, Laste Stojanovski, Ruth Brenk, Julie Frearson, Kevin Read, Ian Gilbert, Paul Wyatt (Lead / Corresponding author)

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Abstract

N-Myristoyltransferase (NMT) represents a promising drug target within the parasitic protozoa Trpanosoma brucei (T. brucei), the causative agent for human African trypanosomiasis (HAT) or sleeping sickness. We have previously validated T. brucei NMT as a promising druggable target for the treatment of HAT in both stage 1 and 2 of the disease. We report on the use of the previously reported DDD85646 (1) as a start point for the design of a class of potent, brain penetrant inhibitors of T. brucei NMT.
Original languageEnglish
Pages (from-to)9790-9806
Number of pages17
JournalJournal of Medicinal Chemistry
Volume60
Issue number23
Early online date10 Nov 2017
DOIs
Publication statusPublished - 14 Dec 2017

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