478929-28-1Relevant academic research and scientific papers
New histamine H3-receptor ligands of the proxifan series: Imoproxifan and other selective antagonists with high oral in vivo potency
Sasse,Sadek,Ligneau,Elz,Pertz,Luger,Ganellin,Arrang,Schwartz,Schunack,Stark
, p. 3335 - 3343 (2000)
Histamine H3-receptor antagonists of the proxifan series are described. The novel compounds possess a 4-(3-(phenoxy)propyl)-1H-imidazole structure and various functional groups, e.g., an oxime moiety, on the phenyl ring. Synthesis of the novel
Decarbonylative Diaryl Ether Synthesis by Pd and Ni Catalysis
Takise, Ryosuke,Isshiki, Ryota,Muto, Kei,Itami, Kenichiro,Yamaguchi, Junichiro
supporting information, p. 3340 - 3343 (2017/03/15)
Because diaryl ethers are present as an important motif in pharmaceuticals and natural products, extensive studies for the development of novel methods have been conducted. A conventional method for the construction of the diaryl ether moiety is the intermolecular cross-coupling reaction of aryl halides and phenols with a copper or palladium catalyst. We developed a catalytic decarbonylative etherification of aromatic esters using a palladium or nickel catalyst with our enabling diphosphine ligand to give the corresponding diaryl ethers. The present reaction can be conducted on gram scale in excellent yield. This reaction not only functions in an intramolecular setting but also allows for a cross-etherification using other phenols.
Aurora isoform selectivity: Design and synthesis of imidazo[4,5- B ]pyridine derivatives as highly selective inhibitors of aurora-A kinase in cells
Bavetsias, Vassilios,Faisal, Amir,Crumpler, Simon,Brown, Nathan,Kosmopoulou, Magda,Joshi, Amar,Atrash, Butrus,Pérez-Fuertes, Yolanda,Schmitt, Jessica A.,Boxall, Katherine J.,Burke, Rosemary,Sun, Chongbo,Avery, Sian,Bush, Katherine,Henley, Alan,Raynaud, Florence I.,Workman, Paul,Bayliss, Richard,Linardopoulos, Spiros,Blagg, Julian
supporting information, p. 9122 - 9135 (2014/01/06)
Aurora-A differs from Aurora-B/C at three positions in the ATP-binding pocket (L215, T217, and R220). Exploiting these differences, crystal structures of ligand-Aurora protein interactions formed the basis of a design principle for imidazo[4,5-b]pyridine-
Design, synthesis and evaluation of galanthamine derivatives as acetylcholinesterase inhibitors
Jia, Ping,Sheng, Rong,Zhang, Jing,Fang, Liang,He, Qiaojun,Yang, Bo,Hu, Yongzhou
experimental part, p. 772 - 784 (2009/09/05)
A new series of galanthamine derivatives have been designed, synthesized and evaluated as acetylcholinesterase inhibitors. All of the new compounds prepared showed high AChE inhibitory activities, with compound 3e that has an N-hexyl-benzyl piperidine substituent on the nitrogen atom reaching the best inhibitory activity for AChE (IC50 = 5.62 nM). The docking study performed with AutoDock demonstrated that 3e was nicely accommodated by AChE.
