The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 6-Bromo-2,3-dihydrobenzo[b][1,4]dioxine(SMILESS: BrC1=CC=C2OCCOC2=C1,cas:52287-51-1) is researched.Formula: C8H7BrO2. The article 《Discovery, optimization, and evaluation of non-bile acid FXR/TGR5 dual agonists》 in relation to this compound, is published in Scientific Reports. Let’s take a look at the latest research on this compound (cas:52287-51-1).
Although several potent bile acid Farnesoid X receptor (FXR) and Takeda G-protein-coupled receptor 5 (TGR5, GPBAR1) dual agonists such as INT-767 have been reported, no non-bile acid FXR/TGR5 dual agonist has been investigated to date. Therefore, we attempted to discover potent non-bile acid FXR/TGR5 dual agonists and identified some non-bile acid FXR/TGR5 dual agonists, such as isonicotinamide derivatives in vitro assay. Compound 20p was evaluated in C57BL/6J mice, that were administered a choline-deficient, L-amino acid-defined, high-fat diet (CDAHFD) consisting of 60 kcal% fat and 0.1% methionine by weight for one week. Compound 20p dose-dependently induced small heterodimer partner (SHP) mRNA and decreased cytochrome P 450 7A1 (CYP7A1) in the liver at 10 and 30 mg/kg, resp., which were used as FXR agonist markers. Compound 20p significantly increased the plasma levels of GLP-1 as a TGR5 agonist, and a high concentration of GLP-1 lowered blood glucose levels. We confirmed that compound 20p was a non-bile acid FXR/TGR5 dual agonist.
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Reference:
Pyrazole – Wikipedia,
Pyrazoles – an overview | ScienceDirect Topics