Design and Synthesis of Brain Penetrant Trypanocidal N-Myristoyltransferase Inhibitors

[Image: see text] 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...

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Detalles Bibliográficos
Autores principales: 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.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2017
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5734605/
https://www.ncbi.nlm.nih.gov/pubmed/29125744
http://dx.doi.org/10.1021/acs.jmedchem.7b01255
Descripción
Sumario:[Image: see text] 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.

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