Umar, Tarana published the artcileA multifunctional therapeutic approach: Synthesis, biological evaluation, crystal structure and molecular docking of diversified 1H-pyrazolo[3,4-b]pyridine derivatives against Alzheimer’s disease, Application of 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine, the main research area is piperazinyl pyrazolopyridinyl acetamide preparation docking cholinesterase inhibitor amyloid aggregation; AChE inhibitors; Amyloid β aggregation inhibitors; Docking; N-(1H-pyrazolo[3,4-b]pyridin-3-yl)acetamides; Selectivity.
2-(Piperazin-1-yl)-N-(1H-pyrazolo[3,4-b]pyridin-3-yl)acetamides I [R = piperidin-1-yl, 4-methylpiperazin-1-yl, Et 4-((4-yl)piperazin-1-yl)quinoline-3-carboxylate, etc.] were described as a new class of selective and potent acetylcholinesterase (AChE) inhibitors and amyloid β aggregation inhibitors. Formation of synthesized compounds I was justified via 1H NMR, 13C NMR, mass spectra and single crystal X-Ray diffraction study. All compounds were evaluated for their acetylcholinesterase and butyrylcholinesterase inhibitory activity, inhibition of self-mediated Aβ aggregation and Cu(II)-mediated Aβ aggregation. Also, docking study was carried out in concordance with in vitro results. The most potent mol. amongst the derivatives exhibited excellent anti-AChE activity (IC50 = 4.8 nM). Kinetic study of I [R = 2-((4-yl)piperazin-1-yl)-N-(1H-pyrazolo[3,4-b]pyridin-3-yl)acetamide] suggested it to be a mixed type inhibitor. In vitro study revealed that all the compounds were capable of inhibiting self-induced β-amyloid (Aβ) aggregation with the highest inhibition percentage to be 81.65%. Potency of I [R = Et 4-((4-yl)piperazin-1-yl)quinoline-3-carboxylate, 2-((4-yl)piperazin-1-yl)-N-(1H-pyrazolo[3,4-b]pyridin-3-yl)acetamide] to inhibit self-induced Aβ1-42 aggregation was ascertained by TEM anal. Compounds were also evaluated for their Aβ disaggregation, antioxidation, metal-chelation activity.
European Journal of Medicinal Chemistry published new progress about Aggregation. 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 of 7-Chloro-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidine.
Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics