학술논문

Synthesis and monoamine oxidase A/B inhibitory evaluation of new benzothiazole-thiazolylhydrazine derivatives.
Document Type
Article
Source
Phosphorus, Sulfur & Silicon & the Related Elements. 2020, Vol. 195 Issue 6, p491-497. 7p.
Subject
*MONOAMINE oxidase
*MASS spectrometry
*BENZOTHIAZOLE
Language
ISSN
1042-6507
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. [ABSTRACT FROM AUTHOR]