微波辅助无溶剂mannich碱的合成、表征及其对HCAⅠ和HCAⅡ同工酶的影响

IF 16.4 1区化学 Q1 CHEMISTRY, MULTIDISCIPLINARY

Accounts of Chemical Research Pub Date : 2021-05-12 DOI:10.20450/MJCCE.2021.1968

B. Büyükkıdan, Nurgün Büyükkıdan, M. Bülbül, M. Yılmaz, Evren Derrun Arslanbay, Ekrem Tunca

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引用次数: 0

摘要

在无溶剂条件下，采用常规微波技术合成了芳香胺的曼尼希碱(2a-d)，并通过IR、NMR (1H、13C)和元素分析对其进行了表征。采用水合酶和酯酶对纯化自人红细胞的碳酸酐酶I和II同工酶(hCA, EC 4.2.1.1)进行体外抑制作用检测。以乙酰唑胺为对照化合物。测定了水合酶和酯酶活性的半数抑制浓度IC50值。只有两种化合物(2b和2d)对酯酶活性表现出较差的hCA I和hCA II抑制作用。相比之下，化合物2a和2c可以作为碳酸酐酶激活剂，因为hCA I和hCA II同工酶的酯酶活性增加。

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Microwave assisted solvent-free mannich bases: synthesis, characterization and effects of these compounds on HCA I and HCA II isozymes

Mannich bases (2a–d) of aromatic amines were synthesized by using a conventional microwave technique under solvent-free conditions and characterized by IR and NMR (1H and 13C) and elemental analysis. The inhibitory effects of the synthesized Mannich bases were examined in vitro by using hydratase and esterase assays on carbonic anhydrase I and II isozymes (hCA, EC 4.2.1.1) purified from human erythrocyte cells. Acetazolamide was used as the control compound. The values of IC50, the half-maximum inhibitory concentration, were found for hydratase and esterase activities. Only two compounds (2b and 2d) exhibited poor hCA I and hCA II inhibition effects on esterase activity. In contrast, compounds 2a and 2c could be used as carbonic anhydrase activators as a result of the increased esterase activity of hCA I and hCA II isozymes.

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来源期刊

Accounts of Chemical Research 化学-化学综合

CiteScore

31.40

自引率

1.10%

发文量

312

审稿时长

2 months

期刊介绍： Accounts of Chemical Research presents short, concise and critical articles offering easy-to-read overviews of basic research and applications in all areas of chemistry and biochemistry. These short reviews focus on research from the author’s own laboratory and are designed to teach the reader about a research project. In addition, Accounts of Chemical Research publishes commentaries that give an informed opinion on a current research problem. Special Issues online are devoted to a single topic of unusual activity and significance. Accounts of Chemical Research replaces the traditional article abstract with an article "Conspectus." These entries synopsize the research affording the reader a closer look at the content and significance of an article. Through this provision of a more detailed description of the article contents, the Conspectus enhances the article's discoverability by search engines and the exposure for the research.