Jameel, Ehtesham published the artcileRational design, synthesis and biological screening of triazine-triazolopyrimidine hybrids as multitarget anti-Alzheimer agents, Application In Synthesis of 24415-66-5, the main research area is triazine triazolopyrimidine preparation antialzheimer antioxidant SAR mol docking human; ADME analysis; Acetylcholinesterase; Alzheimer’s disease; Butyrylcholinesterase; Molecular docking; Triazine; Triazolopyrimidine quinoline.
A series of triazine-triazolopyrimidine hybrids were designed, synthesized and characterized by various spectral techniques. Among the synthesized compounds, the di-substituted triazine-triazolopyrimidine derivatives I (R1 = 3-F3CC6H4NH2, 4-MeOC6H4NH2, 4-FC6H4NH2, 2-FC6H4NH2) showed better acetylcholinesterase (AChE) inhibitory activity than the corresponding tri-substituted triazine-triazolopyrimidine derivatives Out of the disubstituted triazine-triazolopyrimidine based compounds, I (R1 = 3-F3CC6H4NH2) and I (R1 = 4-MeOC6H4NH2) showed encouraging inhibitory activity on AChE with IC50 values 0.065 and 0.092 μM, resp. and they also demonstrated good inhibition selectivity towards AChE over BuChE by ~28 folds. Furthermore, kinetic anal. and mol. modeling studies of these compounds targeted both catalytic active site as well as peripheral anionic site of AChE. In addition, these derivatives effectively modulated Aβ self-aggregation as investigated through CD spectroscopy, ThT fluorescence assay and electron microscopy. Besides, these compounds exhibited potential antioxidant (2.15 and 2.91 trolox equivalent by ORAC assay) and metal chelating properties. In silico ADMET profiling highlighted that, these novel triazine derivatives have appropriate drug like properties and possess very low toxic effects in the primarily pharmacokinetic study. Overall, the multitarget profile exerted by these novel triazine mols. qualified them as potential anti-Alzheimer drug candidates in AD therapy.
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