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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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5734605 | PMC |
| http://dx.doi.org/10.1021/acs.jmedchem.7b01255 | DOI Listing |
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