Investigating the Structure-Activity Relationship of 1,2,4-Triazine G-Protein-Coupled Receptor 84 (GPR84) Antagonists was written by Mahindra, Amit;Jenkins, Laura;Marsango, Sara;Huggett, Mark;Huggett, Margaret;Robinson, Lindsay;Gillespie, Jonathan;Rajamanickam, Muralikrishnan;Morrison, Angus;McElroy, Stuart;Tikhonova, Irina G.;Milligan, Graeme;Jamieson, Andrew G.. And the article was included in Journal of Medicinal Chemistry in 2022.Electric Literature of C3H9NO The following contents are mentioned in the article:
G-protein-coupled receptor 84 (GPR84) is a proinflammatory orphan G-protein-coupled receptor implicated in several inflammatory and fibrotic diseases. Several agonist and antagonist ligands have been developed that target GPR84; however, a noncompetitive receptor blocker that was progressed to phase II clin. trials failed to demonstrate efficacy. New high-quality antagonists are required to investigate the pathophysiol. role of GPR84 and to validate GPR84 as a therapeutic target. Here, authors describe an extensive structure-activity relationship (SAR) of antagonist compound I and also present in silico docking with supporting mutagenesis studies that reveals a potential binding pose for this type of orthosteric antagonist. Lead compound II is a potent GPR84 antagonist with a favorable pharmacokinetic (PK) profile suitable for further drug development. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Electric Literature of C3H9NO).
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. Esterification is the general name for a chemical reaction in which two reactants (typically an alcohol and an acid) form an ester as the reaction product. Esters are common in organic chemistry and biological materials.Electric Literature of C3H9NO
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem