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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Detalles Bibliográficos
Autores principales: 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.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2014
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4269550/
https://www.ncbi.nlm.nih.gov/pubmed/25412409
http://dx.doi.org/10.1021/jm500809c

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