Synthesis and monoamine oxidase A/B inhibitory evaluation of new benzothiazole-thiazolylhydrazine derivatives

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Atıf İçin Kopyala

TURAN G., OSMANİYE D., SAĞLIK B. N., ÇEVİK U. A., LEVENT S., Cavusoglu B. K., ...Daha Fazla

PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS, cilt.195, sa.6, ss.491-497, 2020 (SCI-Expanded)

• Yayın Türü: Makale / Tam Makale
• Cilt numarası: 195 Sayı: 6
• Basım Tarihi: 2020
• Doi Numarası: 10.1080/10426507.2020.1722667
• Dergi Adı: PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS
• Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, Academic Search Premier
• Sayfa Sayıları: ss.491-497
• Eskişehir Osmangazi Üniversitesi Adresli: Hayır

Özet

In this study, a novel series of benzothiazole-thiazolylhydrazine (3a-3i) was synthesized and their structures were characterized by H-1-NMR, C-13-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 mu M). 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 mu M.