618098-56-9

Usage

Uses

Used in Pharmaceutical Industry:
1-(4-FLUOROPHENYL)-3-(4-METHYLPHENYL)-1H-PYRAZOLE-4-CARBALDEHYDE is used as an intermediate in the synthesis of various drugs and pharmaceutical products. Its unique structural features and the presence of fluorophenyl and methylphenyl groups make it a valuable building block for the development of new chemical entities with potential biological activity. This versatility allows for the exploration of diverse chemical reactions and modifications, contributing to its importance in drug discovery and development.

Upstream product

• 1609564-54-6 (E)-1-(4-fluorophenyl)-2-(1-p-tolylethylidene)hydrazine 
• 68-12-2 N,N-dimethyl-formamide 
• 122-00-9 para-methylacetophenone 

Downstream Products

• 956779-12-7 1-(4-fluorophenyl)-3-p-tolyl-1H-pyrazole-4-carboxylic acid 
• 1609564-66-0 1-(4-fluorophenyl)-N-(4-methyl-3-(morpholinosulfonyl)phenyl)-3-p-tolyl-1H-pyrazole-4-carboxamide 

Relevant academic research and scientific papers

FARNESOID X RECEPTOR ANTAGONISTS

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

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.