71280-80-3Relevant academic research and scientific papers
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
Cobalt-Catalyzed Selective Functionalization of Aniline Derivatives with Hexafluoroisopropanol
Zhao, He,Zhao, Shuo,Li, Xiu,Deng, Yinyue,Jiang, Huanfeng,Zhang, Min
supporting information, p. 218 - 222 (2019/01/10)
A cobalt-catalyzed site-selective functionalization of aniline derivatives with hexafluoroisopropanol, which enables the synthesis of a wide array of fluoroalkylated anilines, a class of highly valuable building blocks for further preparation of fluorinated functional products, is reported. The developed transformation proceeds with operational simplicity, use of earth-abundant metal catalyst, broad substrate scope, good functional group tolerance, and mild reaction conditions.
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.
LXR modulators
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Page/Page column 95, (2010/11/26)
A compound of formula I wherein A, X, q, R1, R2a, R2b, R2c, R3a, and R3b are defined herein.
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
Antihypertensive polyfluorohydroxyisopropyl bicyclic and tricyclic carbostyrils
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, (2008/06/13)
Polyfluorohydroxyisopropyl bicyclic and tricyclic carbostyrils, such as 2,3-dihydro-7-methyl-9-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]-5H-pyrido[1,2,3-de]-1,4-benzoxazin-5-one, useful as antihypertensive agents.
