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首页> 外文期刊>Archiv der Pharmazie >Novel sulfamate derivatives of menthol: Synthesis, characterization, and cholinesterases and carbonic anhydrase enzymes inhibition properties
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Novel sulfamate derivatives of menthol: Synthesis, characterization, and cholinesterases and carbonic anhydrase enzymes inhibition properties

机译:薄荷醇的新型亚磺酸衍生物:合成,表征和胆碱酯酶和碳酸酐酶酶抑制性质

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摘要

Abstract Sulfamates have a large spectrum of biological activities including enzyme inhibition. Eight sulfamates derived from menthol ( 2a–h ) were synthesized. Also, in the other section of this study, novel sulfamate derivatives of menthol were tested against some metabolic enzymes including acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and carbonic anhydrase I and II enzymes (hCAs I and II). The newly synthesized novel menthol sulfamate and menthol carbonyl sulfamate derivatives showed K i values in the range of 34.37?±?8.17 to 53.40?±?10.61?nM against hCA I, 12.91?±?4.57 to 38.67?±?6.22?nM against hCA II, 111.17?±?52.36 to 522.86?±?120.08?nM against AChE, and 50.01?±?11.73 to 109.63?±?50.08?nM against BChE. As a result, the novel menthol sulfamate and menthol carbonyl sulfamate derivatives can be promising Alzheimer's disease drug candidates and novel hCA I and hCA II enzymes inhibitors.
机译:摘要磺酸盐具有大谱的生物活性,包括酶抑制。 合成源自薄荷醇(2A-H)的八个磺酸盐。 此外,在本研究的另一部分中,测试薄荷醇的新型巯基衍生物,其对一些代谢酶进行测试,包括乙酰胆碱酯酶(ACHE),丁二醇酸酶(BCHE)和碳酸酐酶I和II酶(HCAs I和II)。 新合成的新型薄荷硫酸和薄荷醇羰基磺胺酸酯衍生物显示出k i值,范围为34.37〜±8.17至53.40〜±10.61Ω·nm,反对HCA I,12.91?±4.57至38.67?±6.22?NM HCA II,111.17?±52.36至522.86?±120.08?nm ache,50.01?±11.73至109.63?±50.08?NM对抗BCHE。 结果,新型薄荷醇氨基甲酸酯和薄荷醇羰基磺酸酯衍生物可承诺阿尔茨海默病药物候选物和新型HCA I和HCA II酶抑制剂。

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