Kumar, Jitendra published the artcileSynthesis and screening of triazolopyrimidine scaffold as multi-functional agents for Alzheimer’s disease therapies, Application In Synthesis of 24415-66-5, the main research area is triazolopyrimidine quinoline hybrid preparation acetylcholinesterase inhibitory activity Alzheimer; cyanopyridine quinoline hybrid preparation acetylcholinesterase inhibitory activity Alzheimer; Acetylcholinesterase; Alzheimer’s disease; Butyrylcholinesterase; Molecular docking; Quinoline; Triazolopyrimidine.
In present study a series of triazolopyrimidine-quinoline and cyanopyridine-quinoline hybrids were designed, synthesized and evaluated as acetylcholinesterase inhibitors (AChEIs). Mol. docking and scoring was utilized for the design of inhibitors. The mols. were synthesized via an easily accessible, convergent synthetic route. Three triazolopyrimidine based compounds showed nanomolar activity towards acetylcholinesterase. Among them, Et 6-fluoro-4-(4-(5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)piperazin-1-yl)quinoline-3-carboxylate (I), strongly inhibited AChE with IC50 value of 42 nM. Furthermore compound I was identified as most promising compound with 12 fold selectivity against butyrylcholinesterase (BuChE). This compound displayed a composed multitargeted profile with promising inhibition of self-induced and AChE – induced Aβ aggregation and antioxidant activity.
European Journal of Medicinal Chemistry published new progress about Alzheimer disease. 24415-66-5 belongs to class triazoles, name is 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine, and the molecular formula is C6H5ClN4, Application In Synthesis of 24415-66-5.
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics