Cargando…
Discovery of Indoline-2-carboxamide Derivatives as a New Class of Brain-Penetrant Inhibitors of Trypanosoma brucei
[Image: see text] There is an urgent need for new, brain penetrant small molecules that target the central nervous system second stage of human African trypanosomiasis (HAT). We report that a series of novel indoline-2-carboxamides have been identified as inhibitors of Trypanosoma brucei from screen...
Autores principales: | Cleghorn, Laura A. T., Albrecht, Sébastien, Stojanovski, Laste, Simeons, Frederick R. J., Norval, Suzanne, Kime, Robert, Collie, Iain T., De Rycker, Manu, Campbell, Lorna, Hallyburton, Irene, Frearson, Julie A., Wyatt, Paul G., Read, Kevin D., Gilbert, Ian H. |
---|---|
Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
American Chemical
Society
2015
|
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4601051/ https://www.ncbi.nlm.nih.gov/pubmed/26418485 http://dx.doi.org/10.1021/acs.jmedchem.5b00596 |
Ejemplares similares
-
Discovery of Inhibitors of Trypanosoma brucei by Phenotypic Screening of a Focused Protein Kinase Library
por: Woodland, Andrew, et al.
Publicado: (2015) -
Optimisation of the Anti-Trypanosoma brucei Activity of the Opioid Agonist U50488
por: Smith, Victoria C, et al.
Publicado: (2011) -
Development of Small-Molecule Trypanosoma brucei N-Myristoyltransferase Inhibitors: Discovery and Optimisation of a Novel Binding Mode
por: Spinks, Daniel, et al.
Publicado: (2015) -
Development
of a 2,4-Diaminothiazole Series for the
Treatment of Human African Trypanosomiasis Highlights the Importance
of Static–Cidal Screening of Analogues
por: Cleghorn, Laura A. T., et al.
Publicado: (2023) -
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
por: Brand, Stephen, et al.
Publicado: (2014)