1037091-16-9Relevant academic research and scientific papers
Potent Thiophene Antagonists of Human Complement C3a Receptor with Anti-Inflammatory Activity
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.
, p. 529 - 541 (2020)
Structure-activity relationships for a series of small-molecule 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 histopathology 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 physiology and disease.
Metal-free deprotonative functionalization of heteroaromatics using organic superbase catalyst
Hirono, Yutaro,Kobayashi, Koji,Yonemoto, Misato,Kondo, Yoshinori
supporting information; experimental part, p. 7623 - 7624 (2010/12/19)
Metal-free deprotonative functionalization of heteroaromatic compounds was achieved using an organic superbase catalyst; an organosilicon additive such as trimethylsilylpropyne was employed for activating the catalytic cycle of 1,2-addition to carbonyl compounds.
MODULATORS OF C3A RECEPTOR AND METHODS OF USE THEREOF
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Page/Page column 161-162, (2008/12/07)
Provided are compounds that are modulators of C3a receptor activity, compositions containing the compounds and methods of use of the compounds and compositions. In certain embodiments, the compounds are pyridones. In certain embodiments, provided are methods for treatment or amelioration of diseases associated with modulation of C3a receptor activity.
