Discovery of a Novel Class of Orally Active Trypanocidal N-Myristoyltransferase Inhibitors

[Image: see text] N-Myristoyltransferase (NMT) represents a promising drug target for human African trypanosomiasis (HAT), which is caused by the parasitic protozoa Trypanosoma brucei. We report the optimization of a high throughput screening hit (1) to give a lead molecule DDD85646 (63), which has...

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Autors principals: Brand, Stephen, Cleghorn, Laura A. T., McElroy, Stuart P., Robinson, David A., Smith, Victoria C., Hallyburton, Irene, Harrison, Justin R., Norcross, Neil R., Spinks, Daniel, Bayliss, Tracy, Norval, Suzanne, Stojanovski, Laste, Torrie, Leah S., Frearson, Julie A., Brenk, Ruth, Fairlamb, Alan H., Ferguson, Michael A. J., Read, Kevin D., Wyatt, Paul G., Gilbert, Ian H.
Format: Artigo
Idioma:Inglês
Publicat: American Chemical Society 2011
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC3256935/
https://ncbi.nlm.nih.gov/pubmed/22148754
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm201091t
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