Publication: N-Substituted Arylidene-3-(Methylsulfonyl)-2-Oxoimidazolidine-1-Carbohydrazide as Cholinesterase Inhibitors: Design, Synthesis, and Molecular Docking Study
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2022-08-01
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Abstract
The development of new enzyme inhibitors in degenerative brain diseases has gained more attention. Enzyme inhibitors play an effective role in controlling central nervous system diseases. For this purpose, a novel series of hydrazone derivatives containing imidazolidine ring aimed against Alzheimer\"s disease (AD), have been designed and synthesized. The acetylcholinesterase (AChE) enzyme inhibitory activity of these compounds was investigated. The structures of the compounds were determined by IR, H-1 and C-13-NMR and mass spectroscopic methods. Inhibition studies on the cholinesterase (ChE) enzymes and beta-amyloid plaque inhibition test of the compounds were performed. Based on the experimental results, compound 3j bearing dimethoxy substituent on the aromatic ring like donepezil exhibited the most AChE inhibitory activity with the IC50 values of 0.023 +/- 0.001 mu M. Owing to obtained biological activity and molecular docking study results, it is thought that the most active compound 3j may play a role in both symptomatic and palliative treatment of AD.
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Yaşam Bilimleri, Moleküler Biyoloji ve Genetik, Sitogenetik, Kimya, Biyokimya, Alkoloidler, Temel Bilimler, Life Sciences, Molecular Biology and Genetics, Cytogenetic, Chemistry, Biochemistry, Alcaloides, Natural Sciences, BİYOKİMYA VE MOLEKÜLER BİYOLOJİ, Moleküler Biyoloji ve Genetik, Yaşam Bilimleri (LIFE), KİMYA, MULTİDİSİPLİNER, Temel Bilimler (SCI), BIOCHEMISTRY & MOLECULAR BIOLOGY, MOLECULAR BIOLOGY & GENETICS, Life Sciences (LIFE), CHEMISTRY, MULTIDISCIPLINARY, CHEMISTRY, Natural Sciences (SCI), Biyokimya, Genetik ve Moleküler Biyoloji (çeşitli), Klinik Biyokimya, Kanser Araştırmaları, Moleküler Biyoloji, İlaç Keşfi, Yaşlanma, Genel Biyokimya, Genetik ve Moleküler Biyoloji, Yapısal Biyoloji, Kimya (çeşitli), Genel Kimya, Fizik Bilimleri, Biochemistry, Genetics and Molecular Biology (miscellaneous), Clinical Biochemistry, Cancer Research, Molecular Biology, Drug Discovery, Aging, General Biochemistry, Genetics and Molecular Biology, Structural Biology, Chemistry (miscellaneous), General Chemistry, Physical Sciences, Alzheimer's disease, beta-amyloid plaque, hydrazone, imidazolidine ring, molecular modeling, BIOLOGICAL EVALUATION, DERIVATIVES BEARING, ANALOGS, MOIETY, β-amyloid plaque
Citation
TOK F., SAĞLIK B. N., ÖZKAY Y., KAPLANCIKLI Z. A., KAYMAKÇIOĞLU B., "N-Substituted Arylidene-3-(Methylsulfonyl)-2-Oxoimidazolidine-1-Carbohydrazide as Cholinesterase Inhibitors: Design, Synthesis, and Molecular Docking Study", CHEMISTRY & BIODIVERSITY, cilt.19, sa.8, 2022