jm7b01255_si_001.pdf (547.49 kB)
Design and Synthesis of Brain Penetrant Trypanocidal N‑Myristoyltransferase Inhibitors
journal contribution
posted on 2017-11-10, 00:00 authored by Tracy Bayliss, David A. Robinson, Victoria C. Smith, Stephen Brand, Stuart P. McElroy, Leah S. Torrie, Chido Mpamhanga, Suzanne Norval, Laste Stojanovski, Ruth Brenk, Julie A. Frearson, Kevin D. Read, Ian H. Gilbert, Paul G. WyattN-Myristoyltransferase
(NMT) represents a promising
drug target within the parasitic protozoa Trypanosoma 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 stages 1 and 2 of the disease. We report on the use
of the previously reported DDD85646 (1) as a starting
point for the design of a class of potent, brain penetrant inhibitors
of T. brucei NMT.