Lead Optimization of a Pyrazole Sulfonamide Series of Trypanosoma bruceiN-Myristoyltransferase Inhibitors: Identification and Evaluation of CNS Penetrant Compounds as Potential Treatments for Stage 2 Human African Trypanosomiasis

[Image: see text] Trypanosoma bruceiN-myristoyltransferase (TbNMT) is an attractive therapeutic target for the treatment of human African trypanosomiasis (HAT). From previous studies, we identified pyrazole sulfonamide, DDD85646 (1), a potent inhibitor of TbNMT. Although this compound represents an...

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Опубликовано в: :J Med Chem
Главные авторы: Brand, Stephen, Norcross, Neil R., Thompson, Stephen, Harrison, Justin R., Smith, Victoria C., Robinson, David A., Torrie, Leah S., McElroy, Stuart P., Hallyburton, Irene, Norval, Suzanne, Scullion, Paul, Stojanovski, Laste, Simeons, Frederick R. C., van Aalten, Daan, Frearson, Julie A., Brenk, Ruth, Fairlamb, Alan H., Ferguson, Michael A. J., Wyatt, Paul G., Gilbert, Ian H., Read, Kevin D.
Формат: Artigo
Язык:Inglês
Опубликовано: American Chemical Society 2014
Online-ссылка:https://ncbi.nlm.nih.gov/pmc/articles/PMC4269550/
https://ncbi.nlm.nih.gov/pubmed/25412409
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm500809c
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