具有α-糖苷酶、乙酰胆碱酯酶、丁酰胆碱酯酶、碳酸酐酶抑制活性的苯丙三醇衍生物的合成与生物评价。
Synthesis and biological evaluation of phloroglucinol derivatives possessing α-glycosidase, acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase inhibitory activity.
机构信息
Faculty of Science, Department of Chemistry, Ataturk University, Erzurum, Turkey.
Tercan Vocational High School, Erzincan University, Erzincan, Turkey.
出版信息
Arch Pharm (Weinheim). 2018 Feb;351(2). doi: 10.1002/ardp.201700314. Epub 2018 Jan 11.
A series of novel phloroglucinol derivatives were designed, synthesized, characterized spectroscopically and tested for their inhibitory activity against selected metabolic enzymes, including α-glycosidase, acetylcholinesterase (AChE), butyrylcholinesterase (BChE), and human carbonic anhydrase I and II (hCA I and II). These compounds displayed nanomolar inhibition levels and showed K values of 1.14-3.92 nM against AChE, 0.24-1.64 nM against BChE, 6.73-51.10 nM against α-glycosidase, 1.80-5.10 nM against hCA I, and 1.14-5.45 nM against hCA II.
一系列新型邻苯三酚衍生物被设计、合成、光谱表征，并测试了它们对选定代谢酶的抑制活性，包括α-糖苷酶、乙酰胆碱酯酶（AChE）、丁酰胆碱酯酶（BChE）以及人碳酸酐酶 I 和 II（hCA I 和 II）。这些化合物表现出纳摩尔抑制水平，并对 AChE 的 K 值为 1.14-3.92 nM，对 BChE 的 K 值为 0.24-1.64 nM，对 α-糖苷酶的 K 值为 6.73-51.10 nM，对 hCA I 的 K 值为 1.80-5.10 nM，对 hCA II 的 K 值为 1.14-5.45 nM。
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