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

Taslimi Parham; Osmanova Sabiya; Gul?in ?lhami; Sardarova Sabira; Farzaliyev Vagif; Sujayev Afsun; Kaya Ruya; Koc Fatma; Beydemir Sukru; Alwasel Saleh H.; Kufrevioglu Omer Irfan

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

机译：有效的碳酸酐酶，乙酰胆碱酯酶和丁酰胆碱酯酶酶抑制剂：新酰胺和噻唑烷-4-苯乙酮碱基

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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 thiazolidine4ones 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 withK i values of 23.76102.75爊M against hCA I, 58.92136.64爊M against hCA II, 1.4012.86爊M against AChE, and 9.8252.77爊M against BChE. On the other hand, acetazolamide showedK i value of 482.63牨?6.20爊M against hCA I, and 1019.60牨?63.70爊M against hCA II. Additionally, Tacrine inhibited AChE and BChE, showingK i values of 397.03牨?1.66 and 210.21牨?5.98爊M, respectively.

机译：含有氮和硫原子的抽象化合物可广泛用于各个领域，包括工业，医药，生物技术和化学技术。其中，酸和杂环化合物的酰胺具有重要的位置。这些酰胺和噻唑烷40元对丁酰基胆碱酯酶（BCHE），乙酰胆碱酯酶（ACHE）和人碳酸酐酶同种型具有良好的抑制作用。疼痛在大脑和红细胞中以高浓度存在。 BCHE是一种在肝脏中丰富的重要酶，它以可溶性形式释放到血液中。他们被证明具有23.76102.75℃的有效的抑制曲线23.76102.75℃，对抗HCA I，58.92136.64℃，对抗HCA II，1.4012.86米对ACHE，而9.8252.77爊M对抗BCHE。另一方面，乙酰唑胺显示出I值482.63‰？6.20℃对HCA I，1019.60‰？63.70爊M对抗HCA II。此外，甲锭抑制疼痛和BCHE，显示I值397.03°+ 1.66和210.21牨？5.98米米。

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来源
《Journal of biochemical and molecular toxicology》 |2017年第9期|共1页
作者
Taslimi Parham; Osmanova Sabiya; Gul?in ?lhami; Sardarova Sabira; Farzaliyev Vagif; Sujayev Afsun; Kaya Ruya; Koc Fatma; Beydemir Sukru; Alwasel Saleh H.; Kufrevioglu Omer Irfan;
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作者单位

Department of Chemistry Faculty of SciencesAtaturk UniversityErzurum 25240 Turkey;

Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives Institute of;

Department of Chemistry Faculty of SciencesAtaturk UniversityErzurum 25240 Turkey;

Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives Institute of;

Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives Institute of;

Laboratory of Theoretical Bases of Synthesis and Action Mechanism of Additives Institute of;

Department of Chemistry Faculty of SciencesAtaturk UniversityErzurum 25240 Turkey;

Department of Chemistry Faculty of SciencesAtaturk UniversityErzurum 25240 Turkey;

Department of Biochemistry Faculty of PharmacyAnadolu UniversityEski?ehir 26470 Turkey;

Department of Zoology College of ScienceKing Saud UniversityRiyadh Saudi Arabia;

Department of Chemistry Faculty of SciencesAtaturk UniversityErzurum 25240 Turkey;

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正文语种 eng
中图分类生物化学;
关键词
acetophenone; acetylcholinesterase; butyrylcholinesterase; carbonic anhydrase; enzyme inhibition;

机译：苯乙酮;乙酰胆碱酯酶;丁酰胆碱酯酶;碳酸酐酶;酶抑制;

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1. Discovery of potent carbonic anhydrase, acetylcholinesterase, and butyrylcholinesterase enzymes inhibitors: The new amides and thiazolidine‐4‐ones synthesized on an acetophenone base [J] . Taslimi Parham, Osmanova Sabiya, Gul?in ?lhami, Journal of biochemical and molecular toxicology . 2017,第9期

机译：有效的碳酸酐酶，乙酰胆碱酯酶和丁酰胆碱酯酶酶抑制剂：新酰胺和噻唑烷-4-苯乙酮碱基
2. Synephrine and phenylephrine act as α‐amylase, α‐glycosidase, acetylcholinesterase, butyrylcholinesterase, and carbonic anhydrase enzymes inhibitors [J] . Taslimi Parham, Ak?nc?oglu Hülya, Gül?in ?lhami Journal of biochemical and molecular toxicology . 2017,第11期

机译：Synephrine和Naphyhrrine充当α-淀粉酶，α-糖苷酶，乙酰胆碱酯酶，丁酰胆碱酯酶和碳酸酐酶酶抑制剂
3. Rosmarinic acid inhibits some metabolic enzymes including glutathione S-transferase, lactoperoxidase, acetylcholinesterase, butyrylcholinesterase and carbonic anhydrase isoenzymes [J] . Gulcin Ilhami, Scozzafava Andrea, Supuran Claudiu T., Journal of enzyme inhibition and medicinal chemistry. . 2016,第4a6期

机译：甘氨酸抑制了一些代谢酶，包括谷胱甘肽S-转移酶，乳酰氧化酶，乙酰胆碱酯酶，丁二醇酸酯酶和碳酸酐酶同工酶
4. Effects of enzyme inhibitors on acetylcholinesterase and detoxification enzymes in Propylaea japonica and Lipaphis erysimi [C] . Chun Yu Kang, Tadashi Miyata, Gang Wu International Diamondback Moth and Other Crucifer Pests Workshop . 2008

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5. Discovery and characterization of potent and selective inhibitors against the PEA-hydrolyzing enzyme, N-acylethanolamine-hydrolyzing acid amidase. [D] . Solorzano Say, Carlos Efrain. 2010

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6. Discovery of Potent Carbonic Anhydrase and Acetylcholinesterase Inhibitors: 2-Aminoindan β-Lactam Derivatives [O] . Hayriye Genç, Ramazan Kalin, Zeynep Köksal, 2016

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7. Rosmarinic acid inhibits some metabolic enzymes including glutathione S-transferase, lactoperoxidase, acetylcholinesterase, butyrylcholinesterase and carbonic anhydrase isoenzymes [O] . İlhami Gülçin, Andrea Scozzafava, Claudiu T. Supuran, 2016

机译：rosmarinic酸抑制一些代谢酶，包括谷胱甘肽S-转移酶，乳酰氧化酶，乙酰胆碱酯酶，丁二醇酸酶和碳酸酐酶同工酶

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

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