Zhu, Junjie published the artcileDesign, synthesis, and structure-activity relationships of 3,4,5-trisubstituted 4,5-dihydro-1,2,4-oxadiazoles as TGR5 agonists in the treatment of type 2 diabetes mellitus and other metabolic disorders, COA of Formula: C8H4ClF3O, the main research area is dihydro oxadiazole preparation TGR5 agonist treatment diabetes metabolic disorder.
Given its role in the mediation of energy and glucose homeostasis, the G-protein-coupled bile acid receptor 1 (TGR5) is considered a potential target for the treatment of type 2 diabetes mellitus and other metabolic disorders. By thorough anal. of diverse structures of published TGR5 agonists, a hypothetical ligand-based pharmacophore model was built, and a new class of potent TGR5 agonists, based on the novel 3,4,5-trisubstituted 4,5-dihydro-1,2,4-oxadiazole core, was discovered by rational design. Three distinct synthetic methods for constructing 4,5-dihydro-1,2,4-oxadiazoles, e.g., I, and extensive structure-activity relationship studies are reported herein. Compound I, the structure of which was determined by single-crystal X-ray diffraction and quantum chem. solid-state TDDFT-ECD calculations, showed the best potency, with an EC50 value of 1.4 nM toward hTGR5. Its favorable properties in vitro warrant further investigation.
ChemMedChem published new progress about Antidiabetic agents. 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, COA of Formula: C8H4ClF3O.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics