Synthesis of 5-trifluoromethyl-2-sulfonylpyridine PPARβ/δ antagonists: Effects on the affinity and selectivity towards PPARβ/δ was written by Kaupang, Aasmund;Kase, Eili Tranheim;Vo, Cecilie Xuan Trang;Amundsen, Marthe;Vik, Anders;Hansen, Trond Vidar. And the article was included in Bioorganic & Medicinal Chemistry in 2016.Recommanded Product: Isoquinoline-1-carboxylic acid This article mentions the following:
The covalent modification of peroxisome-proliferator activated receptor β/δ (PPARβ/δ) is part of the mode of action of 5-trifluoromethyl-2-sulfonylpyridine PPARβ/δ antagonists such as GSK3787 and CC618. Herein, the synthesis and in vitro biol. evaluation of a range of structural analogs of the two antagonists are reported. The new ligands demonstrate that an improvement in the selectivity of 5-trifluoromethyl-2-sulfonylpyridine antagonists towards PPARβ/δ is achievable at the expense of their immediate affinity for PPARβ/δ. However, their putatively covalent and irreversible mode of action may ensure their efficacy over time, as observed in time-resolved fluorescence resonance energy transfer (TR-FRET)-based ligand displacement assays. In the experiment, the researchers used many compounds, for example, Isoquinoline-1-carboxylic acid (cas: 486-73-7Recommanded Product: Isoquinoline-1-carboxylic acid).
Isoquinoline-1-carboxylic acid (cas: 486-73-7) belongs to isoquinoline derivatives. Quinoline and its derivatives are widely used as fungicides, biological agents, antibiotics, alkaloids, dyes, rubber chemicals and flavoring agents. They are also used to make oil-soluble dyes, food colorants, pharmaceuticals, pH indicators and other organic compounds. Recommanded Product: Isoquinoline-1-carboxylic acid
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem