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Synthesis and monoamine oxidase A/B inhibitory evaluation of new benzothiazole-thiazolylhydrazine derivatives
Phosphorus, Sulfur, and Silicon and the Related Elements ( IF 1.3 ) Pub Date : 2020-02-06 , DOI: 10.1080/10426507.2020.1722667 Gülhan Turan 1 , Derya Osmaniye 1, 2 , Begüm Nurpelin Sağlik 1, 2 , Ulviye Acar Çevik 1, 2 , Serkan Levent 1, 2 , Betül Kaya Çavuşoğlu 1, 2 , Ümide Demir Özkay 3 , Yusuf Özkay 1, 2 , Zafer Asım Kaplancikli 1
Phosphorus, Sulfur, and Silicon and the Related Elements ( IF 1.3 ) Pub Date : 2020-02-06 , DOI: 10.1080/10426507.2020.1722667 Gülhan Turan 1 , Derya Osmaniye 1, 2 , Begüm Nurpelin Sağlik 1, 2 , Ulviye Acar Çevik 1, 2 , Serkan Levent 1, 2 , Betül Kaya Çavuşoğlu 1, 2 , Ümide Demir Özkay 3 , Yusuf Özkay 1, 2 , Zafer Asım Kaplancikli 1
Affiliation
Abstract In this study, a novel series of benzothiazole-thiazolylhydrazine (3a–3i) was synthesized and their structures were characterized by 1H-NMR, 13C-NMR spectrometry, and mass spectroscopy. These compounds were evaluated as inhibitors of type A and type B monoamine oxidase (MAO) enzymes. The most active compound 3b (2-((2-(2-(4-(4-Nitrophenyl)thiazol-2-yl)hydrazineylidene)-2-phenylethyl)thio)benzothiazole) showed strong inhibitory activity at hMAO-A (IC50 of 0.095 ± 0.004 µM). Furthermore, compound 3i (2-((2-(2-(4-(2,4-dichlorophenyl)thiazol-2-yl)hydrazineylidene)-2-phenylethyl)thio)benzothiazole) showed significant inhibition profile on hMAO-A with the IC50 values 0.141 ± 0.006 µM. Graphical Abstract
中文翻译：
新型苯并噻唑-噻唑基肼衍生物的合成及单胺氧化酶A/B抑制评价
摘要 本研究合成了一系列新的苯并噻唑-噻唑基肼 (3a-3i)，并通过 1H-NMR、13C-NMR 光谱和质谱对其结构进行了表征。这些化合物被评估为 A 型和 B 型单胺氧化酶 (MAO) 酶的抑制剂。活性最强的化合物 3b (2-((2-(2-(2-(4-(4-Nitrophenyl)thiazol-2-yl)hydrazineylidene)-2-phenylethyl)thio)benzothiazole) 在 hMAO-A (IC50 0.095 ± 0.004 µM）。此外，化合物 3i (2-((2-(2-(4-(2,4-dichlorophenyl)thiazol-2-yl)hydrazineylidene)-2-phenylethyl)thio)benzothiazole 对 hMAO-A 显示出显着的抑制特性IC50 值为 0.141 ± 0.006 µM。图形概要
更新日期：2020-02-06
中文翻译：
新型苯并噻唑-噻唑基肼衍生物的合成及单胺氧化酶A/B抑制评价
摘要 本研究合成了一系列新的苯并噻唑-噻唑基肼 (3a-3i)，并通过 1H-NMR、13C-NMR 光谱和质谱对其结构进行了表征。这些化合物被评估为 A 型和 B 型单胺氧化酶 (MAO) 酶的抑制剂。活性最强的化合物 3b (2-((2-(2-(2-(4-(4-Nitrophenyl)thiazol-2-yl)hydrazineylidene)-2-phenylethyl)thio)benzothiazole) 在 hMAO-A (IC50 0.095 ± 0.004 µM）。此外，化合物 3i (2-((2-(2-(4-(2,4-dichlorophenyl)thiazol-2-yl)hydrazineylidene)-2-phenylethyl)thio)benzothiazole 对 hMAO-A 显示出显着的抑制特性IC50 值为 0.141 ± 0.006 µM。图形概要
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