合成 4,5-二取代-2-硫代-1,2,3,4-四氢嘧啶并[4,5-d]嘧啶-2,4(3H,5H)-二酮并研究其对乙酰胆碱酯酶、丁酰胆碱酯酶、碳酸酐酶 I/II 的抑制作用和抗氧化活性。
Synthesis of 4,5-disubstituted-2-thioxo-1,2,3,4-tetrahydropyrimidines and investigation of their acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase I/II inhibitory and antioxidant activities.
机构信息
a Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives , Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences , Baku , Azerbaijan.
b Department of Chemistry , Faculty of Sciences, Ataturk University , Erzurum , Turkey.
出版信息
J Enzyme Inhib Med Chem. 2016;31(sup3):1-9. doi: 10.1080/14756366.2016.1198901. Epub 2016 Jun 22.
A series of tetrahydropyrimidinethiones were synthesized from thiourea, β-diketones and aromatic aldehydes, such as p-tolualdehyde, p-anisaldehyde, o-tolualdehyde, salicylaldehyde and benzaldehyde. These cyclic thioureas showed good inhibitory action against acetylcholine esterase (AChE), butyrylcholine esterase (BChE), and human (h) carbonic anhydrase (CA) isoforms I and II. AChE and BChE inhibitions were in the range of 6.11-16.13 and 6.76-15.68 nM, respectively. hCA I and II were effectively inhibited by these compounds, with K values in the range of 47.40-76.06 nM for hCA I, and of 30.63-76.06 nM for hCA II, respectively. The antioxidant activity of the cyclic thioureas was investigated by using different in vitro antioxidant assays, including 1,1-diphenyl-2-picrylhydrazyl (DPPH·) radical scavenging, Cuand Fereducing, and Fechelating activities.
一系列四氢嘧啶硫酮是由硫脲、β-二酮和芳香醛如对甲苯醛、对茴香醛、邻甲苯醛、水杨醛和苯甲醛合成的。这些环状硫脲对乙酰胆碱酯酶（AChE）、丁酰胆碱酯酶（BChE）和人（h）碳酸酐酶同工酶 I 和 II 具有良好的抑制作用。AChE 和 BChE 的抑制作用分别在 6.11-16.13 和 6.76-15.68 nM 范围内。这些化合物有效地抑制了 hCA I 和 II，对 hCA I 的 K 值范围为 47.40-76.06 nM，对 hCA II 的 K 值范围为 30.63-76.06 nM。通过使用不同的体外抗氧化测定法，包括 1,1-二苯基-2-苦基肼（DPPH·）自由基清除、Cu 和 Fereducing 以及 Fechelating 活性，研究了环状硫脲的抗氧化活性。
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