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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主要な著者: 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.
フォーマット: Artigo
言語:Inglês
出版事項: American Chemical Society 2011
オンライン･アクセス: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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