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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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: 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
Idioma:Inglês
Publicado em: American Chemical Society 2020
Acesso em linha: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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