Design and Synthesis of Brain Penetrant Trypanocidal N‑Myristoyltransferase Inhibitors

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...

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Bibliographic Details

Published in:	Journal of medicinal chemistry 2017-12, Vol.60 (23), p.9790-9806
Main Authors:	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.
Format:	Article
Language:	eng
Subjects:	Acyltransferases - antagonists & inhibitors Acyltransferases - metabolism Aminopyridines - chemical synthesis Aminopyridines - chemistry Aminopyridines - pharmacokinetics Aminopyridines - pharmacology Animals Brain - metabolism Crystallography, X-Ray Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - pharmacokinetics Enzyme Inhibitors - pharmacology Humans Mice Sulfonamides - chemical synthesis Sulfonamides - chemistry Sulfonamides - pharmacokinetics Sulfonamides - pharmacology Trypanocidal Agents - chemical synthesis Trypanocidal Agents - chemistry Trypanocidal Agents - pharmacokinetics Trypanocidal Agents - pharmacology Trypanosoma brucei brucei - drug effects Trypanosoma brucei brucei - enzymology Trypanosomiasis, African - drug therapy Trypanosomiasis, African - metabolism
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