71280-80-3Relevant articles and documents
Copper(II)-Catalysed Aerobic Oxidative Coupling of Arylamines with Hexafluoroisopropanol: An Alternative Methodology for Constructing Fluorinated Compounds
Guo, Jiabao,Li, Zhanchong,Song, Yang,Wu, Liangying,Yao, Xiaoquan
supporting information, p. 268 - 274 (2020/12/04)
The selective functionalisation of arylamine derivatives with hexafluoroisopropanol through copper(II)-catalysed aerobic oxidative coupling was developed to generate various fluoroalkylated arylamines under mild conditions. This method has a wide substrat
Identification of bicyclic hexafluoroisopropyl alcohol sulfonamides as retinoic acid receptor-related orphan receptor gamma (RORγ/RORc) inverse agonists. Employing structure-based drug design to improve pregnane X receptor (PXR) selectivity
Gong, Hua,Weinstein, David S.,Lu, Zhonghui,Duan, James J.-W.,Stachura, Sylwia,Haque, Lauren,Karmakar, Ananta,Hemagiri, Hemalatha,Raut, Dhanya Kumar,Gupta, Arun Kumar,Khan, Javed,Camac, Dan,Sack, John S.,Pudzianowski, Andrew,Wu, Dauh-Rurng,Yarde, Melissa,Shen, Ding-Ren,Borowski, Virna,Xie, Jenny H.,Sun, Huadong,D'Arienzo, Celia,Dabros, Marta,Galella, Michael A.,Wang, Faye,Weigelt, Carolyn A.,Zhao, Qihong,Foster, William,Somerville, John E.,Salter-Cid, Luisa M.,Barrish, Joel C.,Carter, Percy H.,Dhar, T.G. Murali
, p. 85 - 93 (2017/12/15)
We disclose the optimization of a high throughput screening hit to yield benzothiazine and tetrahydroquinoline sulfonamides as potent RORγt inverse agonists. However, a majority of these compounds showed potent activity against pregnane X receptor (PXR) and modest activity against liver X receptor α (LXRα). Structure-based drug design (SBDD) led to the identification of benzothiazine and tetrahydroquinoline sulfonamide analogs which completely dialed out LXRα activity and were less potent at PXR. Pharmacodynamic (PD) data for compound 35 in an IL-23 induced IL-17 mouse model is discussed along with the implications of a high Ymax in the PXR assay for long term preclinical pharmacokinetic (PK) studies.
Discovery and optimization of a novel series of liver X receptor-α agonists
Li, Leping,Liu, Jiwen,Zhu, Liusheng,Cutler, Serena,Hasegawa, Hirohiko,Shan, Bei,Medina, Julio C.
, p. 1638 - 1642 (2007/10/03)
A novel series of hexafluorocarbinols were discovered as potent activators of the liver X receptor-α using a fluorescence polarization assay. Structure-activity relationship study led to the identification of compounds that are more potent agonists than t
