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强效碳酸酐酶、乙酰胆碱酯酶和丁酰胆碱酯酶抑制剂的发现:基于苯乙酮合成的新型酰胺和噻唑烷-4-酮。

Discovery of potent carbonic anhydrase, acetylcholinesterase, and butyrylcholinesterase enzymes inhibitors: The new amides and thiazolidine-4-ones synthesized on an acetophenone base.

作者信息

Taslimi Parham, Osmanova Sabiya, Gulçin İlhami, Sardarova Sabira, Farzaliyev Vagif, Sujayev Afsun, Kaya Ruya, Koc Fatma, Beydemir Sukru, Alwasel Saleh H, Kufrevioglu Omer Irfan

机构信息

Department of Chemistry, Faculty of Sciences, Ataturk University, Erzurum, 25240, Turkey.

Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives, Institute of Chemistry of Additives, Azerbaijan National Academy of Sciences, Baku, 1029, Azerbaijan.

出版信息

J Biochem Mol Toxicol. 2017 Sep;31(9). doi: 10.1002/jbt.21931. Epub 2017 May 22.

Abstract

Compounds containing nitrogen and sulfur atoms can be widely used in various fields, including industry, medicine, biotechnology, and chemical technology. Among them, amides of acids and heterocyclic compounds have an important place. These amides and thiazolidine-4-ones showed good inhibitory action against butyrylcholinesterase (BChE), acetylcholinesterase (AChE), and human carbonic anhydrase isoforms. AChE exists at high concentrations in the brain and red blood cells. BChE is an important enzyme that is plentiful in the liver, and it is released into the blood in a soluble form. They were demonstrated to have effective inhibition profiles with K values of 23.76-102.75 nM against hCA I, 58.92-136.64 nM against hCA II, 1.40-12.86 nM against AChE, and 9.82-52.77 nM against BChE. On the other hand, acetazolamide showed K value of 482.63 ± 56.20 nM against hCA I, and 1019.60 ± 163.70 nM against hCA II. Additionally, Tacrine inhibited AChE and BChE, showing K values of 397.03 ± 31.66 and 210.21 ± 15.98 nM, respectively.

摘要

含氮和硫原子的化合物可广泛应用于各个领域,包括工业、医学、生物技术和化学技术。其中,酸的酰胺和杂环化合物占有重要地位。这些酰胺和噻唑烷 - 4 - 酮对丁酰胆碱酯酶(BChE)、乙酰胆碱酯酶(AChE)和人类碳酸酐酶同工酶表现出良好的抑制作用。AChE在大脑和红细胞中高浓度存在。BChE是一种重要的酶,在肝脏中大量存在,并以可溶形式释放到血液中。已证明它们对hCA I的K值为23.76 - 102.75 nM、对hCA II的K值为58.92 - 136.64 nM、对AChE的K值为1.40 - 12.86 nM以及对BChE的K值为9.82 - 52.77 nM时具有有效的抑制谱。另一方面,乙酰唑胺对hCA I的K值为482.63 ± 56.20 nM,对hCA II的K值为1019.60 ± 163.70 nM。此外,他克林抑制AChE和BChE,其K值分别为397.03 ± 31.66和210.21 ± 15.98 nM。

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