Usui, Yoshihiro’s team published research in Bioorganic & Medicinal Chemistry Letters in 2017-08-15 | CAS: 452-63-1

Bioorganic & Medicinal Chemistry Letters published new progress about Alzheimer disease (treatment of). 452-63-1 belongs to class bromides-buliding-blocks, name is 1-Bromo-4-fluoro-2-methylbenzene, and the molecular formula is C7H6BrF, Quality Control of 452-63-1.

Usui, Yoshihiro published the artcileDiscovery of novel 2-(3-phenylpiperazin-1-yl)-pyrimidin-4-ones as glycogen synthase kinase-3β inhibitors, Quality Control of 452-63-1, the main research area is phenylpiperazinyl pyrimidinone preparation glycogen synthase kinase inhibitor; Alzheimer’s disease; glycogen synthase kinase-3; phenylpiperazine.

The results of further evolution of glycogen synthase kinase (GSK)-3β inhibitors from authors’ promising compounds containing a 2-phenylmorpholine moiety are described. Transformation of the morpholine moiety into a piperazine moiety resulted in potent GSK-3β inhibitors. SAR studies focused on the Ph moiety revealed that a 4-fluoro-2-methoxy group afforded potent inhibitory activity toward GSK-3β. Based on docking studies of (S)-isomer of I, new hydrogen bonding between the nitrogen atom of the piperazine moiety and the oxygen atom of the main chain of Gln185 has been indicated, which may contribute to increased activity compared with that of the corresponding phenylmorpholine analogs. Effect of the stereochem. of the phenylpiperazine moiety is also discussed.

Bioorganic & Medicinal Chemistry Letters published new progress about Alzheimer disease (treatment of). 452-63-1 belongs to class bromides-buliding-blocks, name is 1-Bromo-4-fluoro-2-methylbenzene, and the molecular formula is C7H6BrF, Quality Control of 452-63-1.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary