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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Detalhes bibliográficos
Publicado no:J Med Chem
Main Authors: 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: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2014
Acesso em linha: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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