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Synthesis of new benzothiazole derivatives bearing thiadiazole as monoamine oxidase inhibitors
Authors:Ulviye Acar Çevik  Derya Osmaniye  Begüm N Sağlik  Serkan Levent  Betül K Çavuşoğlu  Abdullah B Karaduman  Ümide D Özkay  Yusuf Özkay  Zafer A Kaplancikli  Gülhan Turan
Institution:1. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskisehir, Turkey;2. Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, Eskisehir, Turkey

Anadolu University, Faculty of Pharmacy, Doping and Narcotic Compounds Analysis Laboratory, Eskişehir, Turkey;3. Faculty of Pharmacy, Department of Pharmaceutical Toxicology, Anadolu University, Eskisehir, Turkey;4. Department of Pharmacology, Faculty of Pharmacy, Anadolu University, Eskisehir, Turkey

Abstract: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.
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