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首页> 外文期刊>Archiv der Pharmazie >Synthesis and biological evaluation of phloroglucinol derivatives possessing α‐glycosidase, acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase inhibitory activity
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Synthesis and biological evaluation of phloroglucinol derivatives possessing α‐glycosidase, acetylcholinesterase, butyrylcholinesterase, carbonic anhydrase inhibitory activity

机译: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甘油糖醇衍生物的合成与生物学评价

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摘要

Abstract 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 i 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.
机译:摘要设计了一系列新的甘油蛋白衍生物,其特征在一起,表征光谱和测试它们的抑制活性对选定的代谢酶,包括α-糖苷酶,乙酰胆碱酯酶(ACHE),丁酰胆碱酯酶(BCHE)和人碳酸酐酶I和II(HCA I 和ii)。 这些化合物显示纳米摩尔抑制水平,并显示KI值为1.14-3.92Ω·η,0.24-1.64Ω·NM,对抗α-糖苷酶,1.80-5.10≤NM,对抗HCA I和1.14- 5.45?NM对抗HCA II。

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