76856-51-4Relevant academic research and scientific papers
Functional induction of P-glycoprotein efflux pump by phenyl benzenesulfonamides: Synthesis and biological evaluation of T0901317 analogs
Padala, Anil K.,Wani, Abubakar,Vishwakarma, Ram A.,Kumar, Ajay,Bharate, Sandip B.
, p. 744 - 755 (2016)
N-(2,2,2-Trifluoroethyl)-N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-benzenesulfonamide (T0901317, 6) is a potent activator of pregnane-X-receptor (PXR), which is a nuclear receptor controlling P-gp expression. Herein, we aimed to inv
Discovery and optimization of a series of sulfonamide inverse agonists for the retinoic acid receptor-related orphan receptor-α
Doebelin, Christelle,He, Yuanjun,Campbell, Sean,Nuhant, Philippe,Kumar, Naresh,Koenig, Marcel,Garcia-Ordonez, Ruben,Chang, Mi Ra,Roush, William R.,Lin, Li,Kahn, Susan,Cameron, Michael D.,Griffin, Patrick R.,Solt, Laura A.,Kamenecka, Theodore M.
, p. 676 - 684 (2019/10/28)
Background: Despite a massive industry endeavor to develop RORγ-modulators for autoimmune disorders, there has been no indication of efforts to target the close family member RORα for similar indications. This may be due to the misconception that RORα is
Structure-based design of substituted hexafluoroisopropanol- arylsulfonamides as modulators of RORc
Fauber, Benjamin P.,De Leon Boenig, Gladys,Burton, Brenda,Eidenschenk, Celine,Everett, Christine,Gobbi, Alberto,Hymowitz, Sarah G.,Johnson, Adam R.,Liimatta, Marya,Lockey, Peter,Norman, Maxine,Ouyang, Wenjun,Rene, Olivier,Wong, Harvey
supporting information, p. 6604 - 6609 (2014/01/06)
The structure-activity relationships of T0901317 analogs were explored as RORc inverse agonists using the principles of property- and structure-based drug design. An X-ray co-crystal structure of T0901317 and RORc was obtained and provided molecular insight into why T0901317 functioned as an inverse agonist of RORc; whereas, the same ligand functioned as an agonist of FXR, LXR, and PXR. The structural data was also used to design inhibitors with improved RORc biochemical and cellular activities. The improved inhibitors possessed enhanced selectivity profiles (rationalized using the X-ray crystallographic data) against other nuclear receptors.
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
Microwave-induced rapid access to aromatic and heteroaromatic sulfonamides under solvent-free conditions without using external base
Sharma, Ashwani Kumar,Das, Saibal Kumar
, p. 3807 - 3819 (2007/10/03)
Microwave-induced syntheses of sulfonamides, without using base under solvent-free conditions, have been developed. The process finds its utility because of its simple operational procedure and high yields. Moreover, the process is fast and accommodative to different substituents on aromatic as well as heteroaromatic rings rendering sulfonamides (28 examples).
Substituted 4'-polyhaloisopropylsulfonanilides
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, (2008/06/13)
Disclosed are novel substituted 4'-polyhaloisopropylsulfonanilides which are anti-hypertensive agents useful in the treatment of mammalian hypertension. Additionally, the compounds exhibit herbicidal and fungicidal activity. The compounds are prepared by
