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Design, Synthesis, and Biological Effect Studies of Novel Benzofuran-Thiazolylhydrazone Derivatives as Monoamine Oxidase Inhibitors.

ABSTRACT: In recent studies, monoamine oxidase (MAO) inhibitory effects of various thiazolylhydrazone derivatives have been demonstrated. Within the scope of this study, 12 new compounds containing thiazolylhydrazone groups were synthesized. The structures of the obtained compounds were elucidated by 1H NMR, 13C NMR, and high-resolution mass spectrometry (HRMS) methods. The inhibitory effects of the final compounds on MAO enzymes were investigated by means of in vitro methods. In addition to enzyme inhibition studies, enzyme kinetic studies of compounds with high inhibitory activity were examined, and their effects on substrate-enzyme relations were investigated. Additionaly, cytotoxicity tests were carried out to determine the toxicities of the selected compounds, and the compounds were found to be nontoxic. The interactions of the active compound with the active site of the enzyme were characterized by in silico methods.

SUBMITTER: Osmani Ye D 

PROVIDER: S-EPMC10938434 | biostudies-literature | 2024 Mar

REPOSITORIES: biostudies-literature

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Design, Synthesis, and Biological Effect Studies of Novel Benzofuran-Thiazolylhydrazone Derivatives as Monoamine Oxidase Inhibitors.

Osmani Ye Derya D   Sağlik Begüm Nurpelin BN   Levent Serkan S   Çevi K Ulviye Acar UA   Ilgin Sinem S   Yurttaş Leyla L   Özkay Yusuf Y   Karaburun Ahmet Cagri AC   Kaplancikli Zafer Asım ZA   Gundogdu-Karaburun Nalan N  

ACS omega 20240229 10

In recent studies, monoamine oxidase (MAO) inhibitory effects of various thiazolylhydrazone derivatives have been demonstrated. Within the scope of this study, 12 new compounds containing thiazolylhydrazone groups were synthesized. The structures of the obtained compounds were elucidated by <sup>1</sup>H NMR, <sup>13</sup>C NMR, and high-resolution mass spectrometry (HRMS) methods. The inhibitory effects of the final compounds on MAO enzymes were investigated by means of in vitro methods. In add  ...[more]

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