150256-42-1Relevant articles and documents
Expanding the myxochelin natural product family by nicotinic acid containing congeners
Frank, Nicolas A.,Széles, Márió,Akone, Sergi H.,Rasheed, Sari,Hüttel, Stephan,Frewert, Simon,Hamed, Mostafa M.,Herrmann, Jennifer,Schuler, S?ren M. M.,Hirsch, Anna K. H.,Müller, Rolf
supporting information, (2021/08/30)
Myxobacteria represent a viable source of chemically diverse and biologically active secondary metabolites. The myxochelins are a well-studied family of catecholate-type siderophores produced by various myxobacterial strains. Here, we report the discovery
Discovery of Novel Nonpeptidic PAR2 Ligands
Gmeiner, Peter,Hübner, Harald,Kaindl, Jonas,Kl?sel, Ilona,Schmidt, Maximilian F.,Weikert, Dorothee
supporting information, p. 1316 - 1323 (2020/07/04)
Proteinase-activated receptor 2 (PAR2) is a class A G protein-coupled receptor whose activation has been associated with inflammatory diseases and cancer, thus representing a valuable therapeutic target. Pathophysiological roles of PAR2 are often characterized using peptidic PAR2 agonists. Peptidic ligands are frequently unstable in vivo and show poor bioavailability, and only a few approaches toward drug-like nonpeptidic PAR2 ligands have been described. The herein-described ligand 5a (IK187) is a nonpeptidic PAR2 agonist with submicromolar potency in a functional assay reflecting G protein activation. The ligand also showed substantial β-arrestin recruitment. The development of the compound was guided by the crystal structure of PAR2, when the C-terminal end of peptidic agonists was replaced by a small molecule based on a disubstituted phenylene scaffold. IK187 shows preferable metabolic stability and may serve as a lead compound for the development of nonpeptidic drugs addressing PAR2.
Quinazolinones
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Page/Page column 14, (2008/06/13)
Quinazolinones of formula (I) in which R, R1, R2, R3, R4, Y, n and m have the meaning indicated in Patent claim 1, and their salts or solvates as glycoprotein IbIX antagonists