Synthetic Route of 159634-59-0, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.159634-59-0, Name is tert-Butyl 3-oxo-2,3-dihydrospiro[indene-1,4′-piperidine]-1′-carboxylate, molecular formula is C18H23NO3. In a Article£¬once mentioned of 159634-59-0
Scaffold-hopping identifies furano[2,3-d]pyrimidine amides as potent Notum inhibitors
The carboxylesterase Notum is a key negative regulator of the Wnt signaling pathway by mediating the depalmitoleoylation of Wnt proteins. Our objective was to discover potent small molecule inhibitors of Notum suitable for exploring the regulation of Wnt signaling in the central nervous system. Scaffold-hopping from thienopyrimidine acids 1 and 2, supported by X-ray structure determination, identified 3-methylimidazolin-4-one amides 20?24 as potent inhibitors of Notum with activity across three orthogonal assay formats (biochemical, extra-cellular, occupancy). A preferred example 24 demonstrated good stability in mouse microsomes and plasma, and cell permeability in the MDCK-MDR1 assay albeit with modest P-gp mediated efflux. Pharmacokinetic studies with 24 were performed in vivo in mouse with single oral administration of 24 showing good plasma exposure and reasonable CNS penetration. We propose that 24 is a new chemical tool suitable for cellular studies to explore the fundamental biology of Notum.
The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 159634-59-0 is helpful to your research. Synthetic Route of 159634-59-0
Reference£º
Piperidine – Wikipedia,
Piperidine | C5H23139N – PubChem