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首页> 外文期刊>Journal of biochemical and molecular toxicology >Synthesis, characterization, antioxidant, antidiabetic, anticholinergic, and antiepileptic properties of novel N-substituted tetrahydropyrimidines based on phenylthiourea
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Synthesis, characterization, antioxidant, antidiabetic, anticholinergic, and antiepileptic properties of novel N-substituted tetrahydropyrimidines based on phenylthiourea

机译：基于苯硫脲的新型N-取代的四氢嘧啶的合成，表征，抗氧化剂，抗磷酸性能和抗癫痫作用

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摘要

In the presence of trifluoroacetic acid, on the basis of three-component condensation of phenylthiourea with its salicylaldehyde and methyl-3-oxobutanoate, an efficient method for the synthesis of 1-(4-(2-hydroxyphenyl)-6-methyl-1-phenyl-2-thioxo-1,2,3,4-tetrahydropyrimidin-5-yl)ethanone (I) has been worked out. These novel N-substituted tetrahydropyrimidines based on phenylthiourea showed good inhibitory action against acetylcholinesterase (AChE), alpha-glycosidase, and human carbonic anhydrase (hCA) isoforms I and II. K-i values of AChE enzyme were in the range of 0.48 to 7.46 nM. The hCA I and II were effectively inhibited by the compounds, with K-i values in the range of 502.44 to 923.11 nM for hCA I and 400.32 to 801.57 nM for hCA II, respectively. The antioxidant activity of the novel N-substituted tetrahydropyrimidines based on phenylthiourea was investigated by using different in vitro antioxidant assays; including 1,1-diphenyl-2-picrylhydrazyl (DPPH center dot) radical scavenging, Cu2+ and Fe3+ reducing activities.
机译：在三氟乙酸的存在下，基于苯硫脲的三分组分缩合，其水杨醛和甲基-3-氧脱丁酸盐，合成1-（4-（2-羟基苯基）-6-甲基-1的有效方法 - 苯基-2-硫代氧吡啶-5-基）乙烯（I）已经制定出来。基于苯硫脲的这些新的N-取代的四氢嘧啶含有良好的抑制作用对乙酰胆碱酯酶（ACHE），α-糖苷酶和人碳酸酐酶（HCA）同种型I和II的良好抑制作用。疼痛酶的K-I值在0.48至7.46nm的范围内。化合物有效地抑制HCA I和II，k-i值在502.44至923.11nm的范围内，对于HC 3 II分别用于400.32至801.57nm。通过使用不同的体外抗氧化剂测定研究了基于苯硫脲的新型N-取代的四氢嘧啶的抗氧化活性;包括1,1-二苯基-2-富铬酰基（DPPH中心点）自由基清除，Cu2 +和Fe3 +还原活性。

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