Synthesis of new benzothiazole derivatives bearing thiadiazole as monoamine oxidase inhibitors
Monoamine oxidases (MAO) are enzymes that catalyze the oxidative deamination of monoamines such as dopamine, noradrenaline, adrenaline, and serotonin. Recent studies have shown that numerous benzothiazole derivatives exhibit hMAO inhibitory activity in the micromolar concentration range. In this stu...
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| Veröffentlicht in: | Journal of heterocyclic chemistry 2020-05, Vol.57 (5), p.2225-2233 |
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| container_title | Journal of heterocyclic chemistry |
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| creator | Acar Çevik, Ulviye Osmaniye, Derya Sağlik, Begüm N. Levent, Serkan K. Çavuşoğlu, Betül Karaduman, Abdullah B. D. Özkay, Ümide Özkay, Yusuf Kaplancikli, Zafer A. Turan, Gülhan |
| description | Monoamine oxidases (MAO) are enzymes that catalyze the oxidative deamination of monoamines such as dopamine, noradrenaline, adrenaline, and serotonin. Recent studies have shown that numerous benzothiazole derivatives exhibit hMAO inhibitory activity in the micromolar concentration range. In this study, a novel series of benzothiazole‐thiadiazole (5a‐5l) was synthesized and characterized their chemical structures by 1H‐NMR, 13C‐NMR, and Mass spectroscopy. These compounds were evaluated as inhibitors for types A and B MAO enzymes. Compounds 5f and 5l were the most active derivatives in the series with an IC50 values of 0.107 ± 0.003 and 0.128 ± 0.004, respectively. Furthermore, cytotoxicity of compounds 5f and 5l were investigated and found as non‐cytotoxic. |
| doi_str_mv | 10.1002/jhet.3942 |
| format | Article |
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Compounds 5f and 5l were the most active derivatives in the series with an IC50 values of 0.107 ± 0.003 and 0.128 ± 0.004, respectively. 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Compounds 5f and 5l were the most active derivatives in the series with an IC50 values of 0.107 ± 0.003 and 0.128 ± 0.004, respectively. 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| source | Wiley Online Library Journals Frontfile Complete |
| subjects | Chemical synthesis Derivatives Dopamine Enzymes Inhibitors NMR Noradrenaline Nuclear magnetic resonance Serotonin Thiadiazoles Toxicity |
| title | Synthesis of new benzothiazole derivatives bearing thiadiazole as monoamine oxidase inhibitors |
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