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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Λεπτομέρειες βιβλιογραφικής εγγραφής
Τόπος έκδοσης:J Med Chem
Κύριοι συγγραφείς: 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.
Μορφή: Artigo
Γλώσσα:Inglês
Έκδοση: American Chemical Society 2014
Διαθέσιμο Online: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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