Novel Multipotent Amantadine-M30D Hybrids with Highly Selective Butyrylcholinesterase Inhibition and Neuroprotective Effects as Effective Anti-Alzheimer's Agents
| Autor: | Marlyn S. Rada, Wilson Cardona-Galeano, Jorge Quintero-Saumeth, Karina Sierra, Edison Osorio, Luis Alfonso Gonzalez-Molina, Rafael Posada-Duque, Andrés F. Yepes |
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| Rok vydání: | 2022 |
| Předmět: |
N-Methylaspartate
Physiology Cognitive Neuroscience Cell Biology General Medicine Biochemistry Molecular Docking Simulation Structure-Activity Relationship Adenosine Triphosphate Neuroprotective Agents Glutamates Alzheimer Disease Memantine Butyrylcholinesterase Acetylcholinesterase Humans Calcium Cholinesterase Inhibitors |
| Zdroj: | ACS chemical neuroscience. 13(18) |
| ISSN: | 1948-7193 |
| Popis: | As a contribution to the development of new dual/multifunctional drugs, a novel therapeutical scaffold merging key structural features from memantine and M30D was designed, synthesized, and explored for its AChE/BuChE inhibitory activity and neuroprotective effects. All synthetized hybrids were not able to inhibit AChE, but most of them exhibit inhibition with high selectivity toward butyrylcholinesterase (BuChE). Notably, among the tested compounds, amantadine/M30D hybrids with six, seven, nine, and twelve methylene groups in the spacer ( |
| Databáze: | OpenAIRE |
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