Structure-based Discovery of Phenyl (3-Phenylpyrrolidin-3-yl)sulfones as Selective, Orally Active RORγt Inverse Agonists

[Image: see text] A new phenyl (3-phenylpyrrolidin-3-yl)sulfone series of RORγt inverse agonists was discovered utilizing the binding conformation of previously reported bicyclic sulfonamide 1. Through a combination of structure-based design and structure–activity relationship studies, a polar set o...

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Detalhes bibliográficos
Publicado no:ACS Med Chem Lett
Main Authors: Duan, James J.-W., Lu, Zhonghui, Jiang, Bin, Stachura, Sylwia, Weigelt, Carolyn A., Sack, John S., Khan, Javed, Ruzanov, Max, Galella, Michael A., Wu, Dauh-Rurng, Yarde, Melissa, Shen, Ding-Ren, Shuster, David J., Borowski, Virna, Xie, Jenny H., Zhang, Lisa, Vanteru, Sridhar, Gupta, Arun Kumar, Mathur, Arvind, Zhao, Qihong, Foster, William, Salter-Cid, Luisa M., Carter, Percy H., Dhar, T. G. Murali
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2019
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC6421587/
https://ncbi.nlm.nih.gov/pubmed/30891142
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acsmedchemlett.9b00010
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