Synthesis of new derivatives containing pyridine, investigation of MAO inhibitory activities and molecular docking studies
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Derya Osmaniye
,
Begüm Nurpelin Sağlık
,
Serkan Levent
und
Gülhan Turan
Abstract
In this study, novel pyridine-containing thiazolyl hydrazone derivatives were synthesized. Structure determinations of the compounds were performed using 1H NMR, 13C NMR and HRMS techniques. The biological activities of the compounds were evaluated against MAO enzymes by in vitro fluorometric method. As a result of activity studies, compound 3a showed selective inhibitory activity against MAO-B enzyme with IC50 = 0.088 + 0.003 µM. The selectivity index of this compound is greater than 1136. Molecular docking studies were carried out using 2V5Z crystal. It has been observed that docking studies and activity studies are in harmony.
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Author contributions: All the authors have accepted responsibility for the entire content of this submitted manuscript and approved submission.
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Research funding: None declared.
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Conflict of interest statement: The authors declare no conflicts of interest regarding this article.
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Supplementary Material
The online version of this article offers supplementary material (https://doi.org/10.1515/znc-2022-0075).
© 2022 Walter de Gruyter GmbH, Berlin/Boston
Artikel in diesem Heft
- Frontmatter
- Research Articles
- Synthesis, characterization, molecular docking, dynamics simulations, and in silico absorption, distribution, metabolism, and excretion (ADME) studies of new thiazolylhydrazone derivatives as butyrylcholinesterase inhibitors
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- Antidepressant alkaloids from the rhizomes of Corydalis decumbens
- Synthesis of new derivatives containing pyridine, investigation of MAO inhibitory activities and molecular docking studies
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Artikel in diesem Heft
- Frontmatter
- Research Articles
- Synthesis, characterization, molecular docking, dynamics simulations, and in silico absorption, distribution, metabolism, and excretion (ADME) studies of new thiazolylhydrazone derivatives as butyrylcholinesterase inhibitors
- Study on the synthesis and structure-activity relationship of 1,2,3-triazoles against toxic activities of Bothrops jararaca venom
- In-silico elucidation reveals potential phytochemicals against angiotensin-converting enzyme 2 (ACE-2) receptor to fight coronavirus disease 2019 (COVID-19)
- Comparative study of phenolic profile, antioxidant and antimicrobial activities of aqueous extract of white and green tea
- Methylglyoxal and high glucose inhibit VEGFR2 phosphorylation at specific tyrosine residues
- Antidepressant alkaloids from the rhizomes of Corydalis decumbens
- Synthesis of new derivatives containing pyridine, investigation of MAO inhibitory activities and molecular docking studies
- Rapid Communications
- Chemical composition and bioactivities of Magnolia candollii H.Keng essential oil
- Chemical composition and anticholinesterase activity of Lepisanthes rubiginosa (Roxb.) Leenh. essential oil
