Bioevaluation of synthetic pyridones as dual inhibitors of α‐amylase and α‐glucosidase enzymes and potential antioxidants
作者:Faiza Saleem、Khalid Mohammed Khan、Nisar Ullah、Musa Özil、Nimet Baltaş、Shehryar Hameed、Uzma Salar、Abdul Wadood、Ashfaq Ur Rehman、Mukesh Kumar、Muhammad Taha、Syed Moazzam Haider
DOI:10.1002/ardp.202200400
日期:2023.1
Herein, a library of novel pyridone derivatives 1–34 was designed, synthesized, and evaluated for α-amylase and α-glucosidase inhibitory as well as antioxidant activities. Pyridone derivatives 1–34 were synthesized via a one-pot multi-component reaction of variously substituted aromatic aldehydes, acetophenone, ethyl cyanoacetate, and ammonium acetate in absolute ethanol. Synthetic compounds 1–34 were
在此,设计、合成了一个新型吡啶酮衍生物1-34库,并评估了 α-淀粉酶和 α-葡萄糖苷酶抑制以及抗氧化活性。吡啶酮衍生物1-34通过各种取代的芳香醛、苯乙酮、氰基乙酸乙酯和乙酸铵在无水乙醇中的一锅多组分反应合成。通过不同的光谱技术对合成化合物1-34进行了结构表征。大多数测试化合物显示出比标准阿卡波糖(IC 50 = 14.87 ± 0.16 µM)更有希望的抑制潜力,但发现化合物13和12是最有效的化合物,IC 50针对α-淀粉酶和α-葡萄糖苷酶的值分别为 9.20 ± 0.14 µM 和 3.05 ± 0.18 µM。 在 DPPH 自由基清除活性 中,与对照丁基化羟基甲苯 (BHT)(IC 50 = 66.50 ± 0.36 µM)相比,化合物1–34在 IC 50 = 96.50 ± 0.45 至 189.98 ± 1.00 µM范围内也显示出适度的抗氧化潜力。此外,所有合成衍生