New piperidine-hydrazone derivatives: Synthesis, biological evaluations and molecular docking studies as AChE and BChE inhibitors
作者:Nurcan Karaman、Yusuf Sıcak、Tuğba Taşkın-Tok、Mehmet Öztürk、Ayşegül Karaküçük-İyidoğan、Miris Dikmen、Bedia Koçyiğit-Kaymakçıoğlu、Emine Elçin Oruç-Emre
DOI:10.1016/j.ejmech.2016.08.037
日期:2016.11
peroxidation inhibitory activity than the other compounds. In DPPH˙ scavenging assay, compounds 5, 6, 10, 14, 17 demonstrated better activity than that of standard BHT, while in ABTS+˙ scavenging assay compound 6 and 17 exhibited better activity among the other compounds. The CUPRAC assay disclosed that compound 2 displayed better activity than α-tocopherol. The anticholinesterase activity was performed against
drug和含哌啶环的化合物被认为是药物设计中有益的底物。因此,本研究旨在合成由4-氧杂环哌啶-1-羧酸乙酯和2,6-二苯基哌啶-4-酮衍生的新苯甲酰。筛选合成的化合物(1-19)的抗氧化剂,抗胆碱酯酶和抗癌活性。通过使用四个互补试验评估化合物的抗氧化能力。结果表明,化合物7和17具有比其他化合物更高的脂质过氧化抑制活性。在DPPH自由基清除测定中,化合物5,6,10,14,17在ABTS证明比标准BHT的更好的活性,而+˙清除试验化合物6和17在其他化合物中表现出更好的活性。CUPRAC测定法揭示化合物2显示出比α-生育酚更好的活性。抗乙酰胆碱酯酶活性是针对乙酰胆碱酯酶(AChE)和丁酰胆碱酯酶(BChE)酶进行的。化合物11(IC 50:35.30±1.11μM)比加兰他敏(IC 50:46.03± 0.14μM)更好地抑制BChE 。我们得出的结论是,化合物11可以视为BChE抑制