دورية أكاديمية
Exploration of a library of piperonylic acid-derived hydrazones possessing variable aryl functionalities as potent dual cholinesterase and monoamine oxidase inhibitors.
| العنوان: | Exploration of a library of piperonylic acid-derived hydrazones possessing variable aryl functionalities as potent dual cholinesterase and monoamine oxidase inhibitors. |
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| المؤلفون: | Kumar VP; Pharmaceutical Chemistry Research Laboratory II, Department of Pharmaceutical Engineering & Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi, UP, 221005, India., Vishnu MS; Pharmaceutical Chemistry Research Laboratory II, Department of Pharmaceutical Engineering & Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi, UP, 221005, India., Kumar S; Pharmaceutical Chemistry Research Laboratory II, Department of Pharmaceutical Engineering & Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi, UP, 221005, India., Jaiswal S; Pharmaceutical Chemistry Research Laboratory II, Department of Pharmaceutical Engineering & Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi, UP, 221005, India., Ayyannan SR; Pharmaceutical Chemistry Research Laboratory II, Department of Pharmaceutical Engineering & Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi, UP, 221005, India. asraja.phe@iitbhu.ac.in. |
| المصدر: | Molecular diversity [Mol Divers] 2023 Dec; Vol. 27 (6), pp. 2465-2489. Date of Electronic Publication: 2022 Nov 10. |
| نوع المنشور: | Journal Article |
| اللغة: | English |
| بيانات الدورية: | Publisher: ESCOM Science Publishers Country of Publication: Netherlands NLM ID: 9516534 Publication Model: Print-Electronic Cited Medium: Internet ISSN: 1573-501X (Electronic) Linking ISSN: 13811991 NLM ISO Abbreviation: Mol Divers Subsets: MEDLINE |
| أسماء مطبوعة: | Original Publication: Leiden, The Netherlands : ESCOM Science Publishers, c1995- |
| مواضيع طبية MeSH: | Monoamine Oxidase Inhibitors*/pharmacology , Monoamine Oxidase Inhibitors*/chemistry , Cholinesterases*/metabolism, Molecular Docking Simulation ; Hydrazones/pharmacology ; Hydrazones/chemistry ; Kinetics ; Cholinesterase Inhibitors/chemistry ; Monoamine Oxidase/chemistry ; Structure-Activity Relationship ; Acetylcholinesterase/metabolism |
| مستخلص: | A library of piperonylic acid-derived hydrazones possessing variable aryl moiety was synthesized and investigated for their multifunctional properties against cholinesterases (ChEs) and monoamine oxidases (MAOs). The in vitro enzymatic assay results revealed that the tested hydrazones have exhibited excellent cholinesterase inhibition profile. Compound 4i, (E)-N'-(2,3-dichlorobenzylidene)benzo[d][1,3]dioxole-5-carbohydrazide showed promising dual inhibitory profile against AChE (0.048 ± 0.007 μM), BChE (0.89 ± 0.018 μM), and MAO-B (0.95 ± 0.12 μM) enzymes. SAR exploration revealed that the truncation of the linker connecting both the aryl binding sites of the semicarbazone scaffold, by one atom, has relatively suppressed the AChE inhibitory potential. Kinetic studies disclosed that the compound 4i reversibly inhibited AChE enzyme in a competitive manner (K (© 2022. The Author(s), under exclusive licence to Springer Nature Switzerland AG.) |
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| فهرسة مساهمة: | Keywords: Cholinesterase; Dual inhibitors; Hydrazones; Molecular docking; Monoamine oxidase; Piperonylic acid |
| المشرفين على المادة: | 0 (Monoamine Oxidase Inhibitors) EC 3.1.1.8 (Cholinesterases) QX3V1NO0KH (piperonylic acid) 0 (Hydrazones) 103-47-9 (2-(N-cyclohexylamino)ethanesulfonic acid) 0 (Cholinesterase Inhibitors) EC 1.4.3.4 (Monoamine Oxidase) EC 3.1.1.7 (Acetylcholinesterase) |
| تواريخ الأحداث: | Date Created: 20221110 Date Completed: 20231113 Latest Revision: 20231113 |
| رمز التحديث: | 20231215 |
| DOI: | 10.1007/s11030-022-10564-9 |
| PMID: | 36355337 |
| قاعدة البيانات: | MEDLINE |
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Full Text Finder | تدمد: | 1573-501X |
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| DOI: | 10.1007/s11030-022-10564-9 |