Potent Thiophene Antagonists of Human Complement C3a Receptor with Anti-Inflammatory Activity was written by Rowley, Jessica A.;Reid, Robert C.;Poon, Eunice K. Y.;Wu, Kai-Chen;Lim, Junxian;Lohman, Rink-Jan;Hamidon, Johan K.;Yau, Mei-Kwan;Halili, Maria A.;Durek, Thomas;Iyer, Abishek;Fairlie, David P.. And the article was included in Journal of Medicinal Chemistry in 2020.SDS of cas: 91-02-1 This article mentions the following:
Structure-activity relationships for a series of small-mol. thiophenes resulted in potent and selective antagonism of human Complement C3a receptor. The compounds are about 100-fold more potent than the most reported antagonist SB290157. A new compound JR14a was among the most potent of the new antagonists in vitro, assessed by (a) inhibition of intracellular calcium release (IC50 10 nM) induced in human monocyte-derived macrophages by 100 nM C3a, (b) inhibition of β-hexosaminidase secretion (IC50 8 nM) from human LAD2 mast cells degranulated by 100 nM C3a, and (c) selectivity for human C3aR over C5aR. JR14a was metabolically stable in rat plasma and in rat liver microsomes and efficacious in rats when given orally to suppress rat paw inflammation, macrophage and mast cell activation, and histopathol. induced by intraplantar paw administration of a C3aR agonist. Potent C3aR antagonists are now available for interrogating C3a receptor activation and suppressing C3aR-mediated inflammation in mammalian physiol. and disease. In the experiment, the researchers used many compounds, for example, Phenyl(pyridin-2-yl)methanone (cas: 91-02-1SDS of cas: 91-02-1).
Phenyl(pyridin-2-yl)methanone (cas: 91-02-1) belongs to pyridine derivatives. In contrast to benzene, Pyridine’s electron density is not evenly distributed over the ring, reflecting the negative inductive effect of the nitrogen atom. Reduced pyridines, namely tetrahydropyridines, dihydropyridines and piperidines, are found in numerous natural and synthetic compounds. The synthesis and reactivity of these compounds have often been driven by the fact many of these compounds have interesting and unique pharmacological properties. SDS of cas: 91-02-1