Ulven, Elisabeth Rexen; Quon, Tezz; Sergeev, Eugenia; Barki, Natasja; Brvar, Matjaz; Hudson, Brian D.; Dutta, Palash; Hansen, Anders Hoejgaard; Bielefeldt, Line Oe.; Tobin, Andrew B.; McKenzie, Christine J.; Milligan, Graeme; Ulven, Trond published the artcile< Structure-Activity Relationship Studies of Tetrahydroquinolone Free Fatty Acid Receptor 3 Modulators>, COA of Formula: C4H3NOS, the main research area is fatty acid receptor FFAR3 tetrahydroquinolone allosteric modulator.
Free fatty acid receptor 3 (FFA3, previously GPR41) is activated by short-chain fatty acids, mediates health effects of the gut microbiota, and is a therapeutic target for metabolic and inflammatory diseases. The shortage of well-characterized tool compounds has however impeded progress. Herein, we report structure-activity relationship of an allosteric modulator series and characterization of physicochem. and pharmacokinetic properties of selected compounds, including previous and new tools. Two representatives, 57 (TUG-1907) and 63 (TUG-2015), showed improved solubility and preserved potency. Of these, 57, with EC50 = 145 nM and a solubility of 33μM, showed high clearance in vivo but is a preferred tool in vitro. In contrast, 63, with EC50 = 162 nM and a solubility of 9μM, showed lower clearance and seems better suited for in vivo studies. Using 57, we demonstrate for the first time that FFA3 activation leads to calcium mobilization in murine dorsal root ganglia.
Journal of Medicinal Chemistry published new progress about Allosteric modulators. 1003-32-3 belongs to class thiazole, and the molecular formula is C4H3NOS, COA of Formula: C4H3NOS.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica