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一些吡唑衍生物:碳酸酐酶、α-糖苷酶和胆碱酯酶的有效抑制剂。

Some pyrazoles derivatives: Potent carbonic anhydrase, α-glycosidase, and cholinesterase enzymes inhibitors.

机构信息

Health Services Vocational School, Igdır University, Igdır, Turkey.

Faculty of Education, Department of Science, Muş Alparslan University, Muş, Turkey.

出版信息

Arch Pharm (Weinheim). 2018 Oct;351(10):e1800200. doi: 10.1002/ardp.201800200. Epub 2018 Sep 23.

Abstract

A series of substituteed pyrazol-4-yl-diazene derivatives were found to be effective inhibitors against α-glycosidase, cytosolic carbonic anhydrase I and II isoforms (hCA I and II), butyrylcholinesterase (BChE), and acetylcholinesterase (AChE) with K values in the range of 33.72 ± 7.93 to 90.56 ± 27.52 nM for α-glycosidase, 1.06 ± 0.16 to 9.83 ± 0.74 nM for hCA I, 0.68 ± 0.12 to 7.16 ± 1.14 nM for hCA II, 44.66 ± 10.06 to 78.34 ± 17.83 nM for AChE, and 50.36 ± 13.88 to 88.36 ± 20.03 nM for BChE, respectively. Recently, inhibition of these metabolic enzymes has been considered as a promising factor for pharmacologic intervention in a diversity of disturbances, such as diabetes, glaucoma, obesity, epilepsy, cancer, and neurodegenerative diseases.

摘要

一系列取代的吡唑-4-基二氮烯衍生物被发现是有效的α-糖苷酶、细胞溶质碳酸酐酶 I 和 II 同工型(hCA I 和 II)、丁酰胆碱酯酶(BChE)和乙酰胆碱酯酶(AChE)抑制剂,其 K 值范围为 33.72±7.93 至 90.56±27.52 nM 用于 α-糖苷酶,1.06±0.16 至 9.83±0.74 nM 用于 hCA I,0.68±0.12 至 7.16±1.14 nM 用于 hCA II,44.66±10.06 至 78.34±17.83 nM 用于 AChE,50.36±13.88 至 88.36±20.03 nM 用于 BChE。最近,这些代谢酶的抑制作用被认为是在多种紊乱中进行药理干预的一个很有前途的因素,如糖尿病、青光眼、肥胖症、癫痫、癌症和神经退行性疾病。

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