Discovery of the S1P2 Antagonist GLPG2938 (1-[2-Ethoxy-6-(trifluoromethyl)-4-pyridyl]-3-[[5-methyl-6-[1-methyl-3-(trifluoromethyl)pyrazol-4-yl]pyridazin-3-yl]methyl]urea), a Preclinical Candidate for the Treatment of Idiopathic Pulmonary Fibrosis was written by Mammoliti, Oscar;Palisse, Adeline;Joannesse, Caroline;El Bkassiny, Sandy;Allart, Brigitte;Jaunet, Alex;Menet, Christel;Coornaert, Beatrice;Sonck, Kathleen;Duys, Inge;Clement-Lacroix, Philippe;Oste, Line;Borgonovi, Monica;Wakselman, Emanuelle;Christophe, Thierry;Houvenaghel, Nicolas;Jans, Mia;Heckmann, Bertrand;Saniere, Laurent;Brys, Reginald. And the article was included in Journal of Medicinal Chemistry in 2021.Recommanded Product: 109-85-3 The following contents are mentioned in the article:
Mounting evidence from the literature suggests that blocking S1P2 receptor (S1PR2) signaling could be effective for the treatment of idiopathic pulmonary fibrosis (IPF). However, only a few antagonists have been so far disclosed. A chem. enablement strategy led to the discovery of a pyridine series with good antagonist activity. A pyridazine series with improved lipophilic efficiency and with no CYP inhibition liability was identified by scaffold hopping. Further optimization led to the discovery of 40 (GLPG2938)(I), a compound with exquisite potency on a phenotypic IL8 release assay, good pharmacokinetics, and good activity in a bleomycin-induced model of pulmonary fibrosis. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Recommanded Product: 109-85-3).
2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits, including apples, durians, pears, bananas, pineapples, and strawberries. Acyl chlorides and acid anhydrides alcoholysis is another way to produce esters. Acyl chlorides and acid anhydrides react with alcohols to produce esters. Anydrous conditions are recommended since both acyl chlorides and acid anhydrides react with water.Recommanded Product: 109-85-3
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem