Bayliss Tracy, Robinson David A, Smith Victoria C, Brand Stephen, McElroy Stuart P, Torrie Leah S, Mpamhanga Chido, Norval Suzanne, Stojanovski Laste, Brenk Ruth, Frearson Julie A, Read Kevin D, Gilbert Ian H, Wyatt Paul G
Drug Discovery Unit, College of Life Sciences, University of Dundee , Sir James Black Centre, Dundee DD1 5EH, U.K.
J Med Chem. 2017 Dec 14;60(23):9790-9806. doi: 10.1021/acs.jmedchem.7b01255. Epub 2017 Nov 22.
N-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.
N-肉豆蔻酰转移酶（NMT）是寄生原生动物布氏锥虫（导致人类非洲锥虫病，即昏睡病的病原体）中一个很有前景的药物靶点。我们之前已证实布氏锥虫NMT是治疗昏睡病1期和2期的一个很有前景的可成药靶点。我们报道了以之前报道的DDD85646（1）为起点来设计一类强效、可穿透血脑屏障的布氏锥虫NMT抑制剂。
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