Kumar, Jitendra published the artcilePyrimidine-Triazolopyrimidine and Pyrimidine-Pyridine Hybrids as Potential Acetylcholinesterase Inhibitors for Alzheimer’s Disease, Name: 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine, the main research area is pyrimidine triazolopyrimidine preparation Alzheimer disease acetylcholinesterase inhibitor.
Synthesis and testing of pyrimidine derivatives in conjugation with triazolopyrimidine I [R = [(6-bromonaphthalen-2-yl)oxy], (4-nitrophenyl)aminyl, (naphthalen-2-yloxy)] based hybrid scaffold of AChE inhibitors for development of new mols. towards the treatment of AD were reported. A multipronged approach employing computational, chem. and biol. approaches was used to find the best inhibitor of AChE. Three mols. (2-(4-(6-chloropyrimidin-4-yl)piperazin-1-yl)nicotinonitrile, I (R = [(6-bromonaphthalen-2-yl)oxy]) and II) derived from this scaffold inhibited AChE in nanomolar to micromolar range. Highest activity was shown by II which has IC50 value of 36 nM. Inhibitory effect of II was stronger for human AChE in neuronal cell extract compared to eelAChE. This activity is comparable to donepezil (IC50 = 38nM) which is considered as good standard among AChE inhibitors. The inhibitory activity of II was also in agreement with mol. simulation studies which showed stable interaction of the II with the catalytic active site as well as peripheral anionic site. Mol. simulation studies also indicated stronger interaction of II with rhAChE than TcAChE. This was later confirmed in studies with neuronal cell extract where compound II showed enzyme inhibition at 25 nM. Further this mol. was not found to be toxic or carcinogenic.
ChemistrySelect 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, Name: 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine.
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics