A novel series of flavonoid based compounds were designed, synthesized and biologically evaluated for Acetylcholinesterase (AChE) inhibitory activity integrated with advanced glycation end products (AGEs) inhibitory and antioxidant potential. Most of the derivatives inhibited AChE in nanomolar IC₅₀ range along with good AGEs inhibitory and radical scavenging activity. Among them, 7m, strongly inhibited AChE (IC₅₀ = 5.87 nM) and found to be potent as compared to the reference drug donepezil (IC₅₀ = 12.7 nM). Its potent inhibitory activity has been justified by docking analysis that revealed its dual binding characteristic with both CAS (catalytic active site) and PAS (peripheral anionic site) of AChE, simultaneously. Additionally, this compound also displayed ability to prevent advanced glycation end products formation (IC₅₀ = 23.0 µM) with additional radical scavenging property (IC₅₀ = 37.12 nM). It (7m) also ameliorated scopolamine induced memory deficit in mice employing Morris water maze test. Thus, flavonoids might be the promising lead compounds as potential polyfunctional anti-Alzheimer’s agents.

设计，合成和生物评估了一系列基于类黄酮的新型化合物，并结合了先进的糖基化终产物（AGEs）抑制和抗氧化潜力，对乙酰胆碱酯酶（AChE）的抑制活性进行了生物学评估。大多数衍生物在纳摩尔IC ₅₀范围内均能抑制AChE，并具有良好的AGEs抑制和自由基清除活性。其中7m强烈抑制AChE（IC ₅₀  = 5.87 nM），并且与参考药物多奈哌齐（IC _50）相比具有较强的抑制作用。 = 12.7 nM）。通过对接分析证明了其有效的抑制活性，该对接分析揭示了其与AChE的CAS（催化活性位点）和PAS（外围阴离子位点）同时具有双重结合特性。此外，该化合物还具有防止晚期糖基化终产物形成的能力（IC ₅₀  = 23.0 µM），并具有额外的自由基清除性能（IC ₅₀  = 37.12 nM）。它（7m）还通过使用莫里斯水迷宫试验改善了东pol碱引起的小鼠记忆力减退。因此，类黄酮作为潜在的多官能抗阿尔茨海默氏病药物可能是有前途的先导化合物。