929032-56-4Relevant 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 (2020/02/05)
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.
Palladium-catalyzed benzylation of heterocyclic aromatic compounds
Lapointe, David,Fagnou, Keith
supporting information; experimental part, p. 4160 - 4163 (2009/12/07)
Broadly applicable palladium-catalyzed heteroarene benzylation reactions are described with a focus on the most challenging heterocyclic classes under traditional benzylation techniques such as sulfur-containing heterocycles and those bearing functional groups that would be incompatible with reactions requiring Lewis acids and/or strong bases.
Novel acyl hydrazino thiophene derivatives, process for preparing them, their use as medicinal products, pharmaceutical compositions and novel use
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Page/Page column 19, (2010/02/12)
The invention concerns novel compounds of formula (I), process for making, pharmaceutical compositions and methods of treating diseases associated with abnormal physiological behavior in the secretion and/or the activity of cysteine proteases especially c
