Design, synthesis, acetylcholinesterase, butyrylcholinesterase, and amyloid‐β aggregation inhibition studies of substituted 4,4ʹ‐diimine/4,4ʹ‐diazobiphenyl derivatives
作者:Görkem S. Fidan、Sulunay Parlar、Ayse H. Tarikogullari、Vildan Alptuzun、Ayşe S. Alpan
DOI:10.1002/ardp.202200152
日期:2022.12
displayed weak or no BChE inhibition. Among the title compounds, compound 2l, 4,4′-bis(quinolin-8-yldiazenyl)-1,1′-biphenyl, having a diazo-quinoline moiety demonstrated the most potent inhibition against AChE with an IC50 value of 5.77 μM. Furthermore, diazo derivatives 2d, 4,4′-bis[(4-methoxyphenyl)diazenyl]-1,1′-biphenyl, and 2i, 4,4′-bis(pyridin-3-yldiazenyl)-1,1′-biphenyl, provided better potency on Aβ1–42
设计、合成了一系列 4,4'-二亚胺/4,4'-重氮联苯衍生物,并评估了它们抑制乙酰胆碱酯酶 (AChE) 和丁酰胆碱酯酶 (BChE) 酶以及 Aβ 1–42聚集的能力,体外。AChE 和 BChE 抑制测定表明,所有化合物在 IC 50 = 5.77–16.22 μM 范围内均显示出中度 AChE 抑制活性,而它们显示出较弱或无 BChE 抑制作用。在标题化合物中,化合物2l , 4,4'-bis(quinolin-8-yldiazenyl)-1,1'-biphenyl, having a diazo-quinoline moiety 证明对 AChE 的抑制作用最强,IC 50值为 5.77 μM . 此外,重氮衍生物2d, 4,4'-bis[(4-methoxyphenyl)diazenyl]-1,1'-biphenyl, and 2i , 4,4'-bis(pyridin-3-yldiazenyl)-1