Aksu Kadir, Özgeriş Bünyamin, Taslimi Parham, Naderi Ali, Gülçin İlhami, Göksu Süleyman
Faculty of Arts and Sciences, Department of Chemistry, Ordu University, Ordu, Turkey.
Faculty of Science, Department of Basic Sciences, Erzurum Technical University, Erzurum, Turkey.
Arch Pharm (Weinheim). 2016 Dec;349(12):944-954. doi: 10.1002/ardp.201600183. Epub 2016 Nov 10.
A series of ureas derived from phenethylamines were synthesized and evaluated for human carbonic anhydrase (hCA) I and II, acetylcholinesterase (AChE), and butyrylcholinesterase (BChE) enzyme inhibitory activities and antioxidant properties. The ureas were synthesized from the reactions of substituted phenethylamines with N,N-dimethylcarbamoyl chloride; then, the synthesized compounds were converted to their corresponding phenolic derivatives via O-demethylation. hCA I and II were effectively inhibited by the newly synthesized compounds, with K values in the range of 0.307-0.432 nM for hCA I and 0.149-0.278 nM for hCA II. On the other hand, the K parameters of these compounds for AChE and BChE were determined in the range of 0.129-0.434 and 0.095-0.207 nM, respectively. Phenolic ureas also showed good antioxidant activities.
合成了一系列源自苯乙胺的脲类化合物,并对其进行了人碳酸酐酶(hCA)I和II、乙酰胆碱酯酶(AChE)以及丁酰胆碱酯酶(BChE)的酶抑制活性和抗氧化性能评估。这些脲类化合物由取代苯乙胺与N,N - 二甲基甲酰氯反应合成;然后,通过O - 去甲基化将合成的化合物转化为其相应的酚类衍生物。新合成的化合物能有效抑制hCA I和II,hCA I的K值范围为0.307 - 0.432 nM,hCA II的K值范围为0.149 - 0.278 nM。另一方面,这些化合物对AChE和BChE的K参数分别在0.129 - 0.434和0.095 - 0.207 nM范围内。酚类脲也表现出良好的抗氧化活性。