342026-17-9Relevant academic research and scientific papers
FARNESOID X RECEPTOR ANTAGONISTS
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, (2015/09/23)
Provided herein are Farnesoid X receptor (FXR) antagonists, methods of antagonizing FXR, and methods of treating metabolic disease using the antagonists herein.
Identification of trisubstituted-pyrazol carboxamide analogs as novel and potent antagonists of farnesoid X receptor
Yu, Donna D.,Lin, Wenwei,Forman, Barry M.,Chen, Taosheng
, p. 2919 - 2938 (2014/05/20)
Farnesoid X receptor (FXR, NRIH4) plays a major role in the control of cholesterol metabolism. This suggests that antagonizing the transcriptional activity of FXR is a potential means to treat cholestasis and related metabolic disorders. Here we describe the synthesis, biological evaluation, and structure-activity relationship (SAR) studies of trisubstituted-pyrazol carboxamides as novel and potent FXR antagonists. One of these novel FXR antagonists, 4j has an IC50 of 7.5 nM in an FXR binding assay and 468.5 nM in a cell-based FXR antagonistic assay. Compound 4j has no detectable FXR agonistic activity or cytotoxicity. Notably, 4j is the most potent FXR antagonist identified to date; it has a promising in vitro profile and could serve as an excellent chemical tool to elucidate the biological function of FXR.
Solid-phase synthesis of amino acid derived N-unsubstituted pyrazoles via sydnones
Harju, Kirsi,Vesterinen, Johanna,Yli-Kauhaluoma, Jari
supporting information; experimental part, p. 2219 - 2221 (2009/09/28)
A new method to synthesize N-unsubstituted pyrazoles on a solid support is described. The solid support acts as a protecting group for the amino acid. N-Protected amino acid is N-nitrosated, and the subsequent treatment with acetic anhydride in a microwav
AMIDE COMPOUNDS
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Page/Page column 255-256, (2008/06/13)
The present invention provides compounds represented by the formula (Ia) the formula (Ib) the formula (Ic) and the formula (Id) wherein each symbol is as defined in the specification. According to the present invention, these compounds have a DGAT inhibit
