Novel Tricyclic Pyroglutamide Derivatives as Potent RORγt Inverse Agonists Identified using a Virtual Screening Approach

[Image: see text] Employing a virtual screening approach, we identified the pyroglutamide moiety as a nonacid replacement for the cyclohexanecarboxylic acid group which, when coupled to our previously reported conformationally locked tricyclic core, provided potent and selective RORγt inverse agonis...

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Publicado en:ACS Med Chem Lett
Autores principales: Liu, Qingjie, Batt, Douglas G., Weigelt, Carolyn A., Yip, Shiuhang, Wu, Dauh-Rurng, Ruzanov, Max, Sack, John S., Wang, Jinhong, Yarde, Melissa, Li, Sha, Shuster, David J., Xie, Jenny H., Sherry, Tara, Obermeier, Mary T., Fura, Aberra, Stefanski, Kevin, Cornelius, Georgia, Khandelwal, Purnima, Tino, Joseph A., Macor, John E., Salter-Cid, Luisa, Denton, Rex, Zhao, Qihong, Dhar, T. G. Murali
Formato: Artigo
Lenguaje:Inglês
Publicado: American Chemical Society 2020
Acceso en línea:https://ncbi.nlm.nih.gov/pmc/articles/PMC7734821/
https://ncbi.nlm.nih.gov/pubmed/33335675
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.0c00496
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