Evaluation of 5-(Trifluoromethyl)-1,2,4-oxadiazole-Based Class IIa HDAC Inhibitors for Huntington’s Disease

[Image: see text] Using an iterative structure–activity relationship driven approach, we identified a CNS-penetrant 5-(trifluoromethyl)-1,2,4-oxadiazole (TFMO, 12) with a pharmacokinetic profile suitable for probing class IIa histone deacetylase (HDAC) inhibition in vivo. Given the lack of understan...

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Publicat a:ACS Med Chem Lett
Autors principals: Stott, Andrew J., Maillard, Michel C., Beaumont, Vahri, Allcock, David, Aziz, Omar, Borchers, Alexander H., Blackaby, Wesley, Breccia, Perla, Creighton-Gutteridge, Gillian, Haughan, Alan F., Jarvis, Rebecca E., Luckhurst, Christopher A., Matthews, Kim L., McAllister, George, Pollack, Scott, Saville-Stones, Elizabeth, Van de Poël, Amanda J., Vater, Huw D., Vann, Julie, Williams, Rachel, Yates, Dawn, Muñoz-Sanjuán, Ignacio, Dominguez, Celia
Format: Artigo
Idioma:Inglês
Publicat: American Chemical Society 2021
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC7957923/
https://ncbi.nlm.nih.gov/pubmed/33738065
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.0c00532
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