Development of novel salicylic acid-donepezil-rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer's disease
Alzheimer's disease (AD) is a chronic, progressive brain degenerative disease that is common in the elderly. So far, there is no effective treatment. The multi-target-directed ligands (MTDLs) strategy has been recognised as the most promising approach due to the complexity of the pathogenesis o...
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| Main Authors: | , , , , , , , , , |
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Taylor & Francis Group,
2023-12-01T00:00:00Z.
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| 001 | doaj_01e902f90d2041f1bf78b8a7c5596af2 | ||
| 042 | |a dc | ||
| 100 | 1 | 0 | |a Yi Zhou |e author |
| 700 | 1 | 0 | |a Ying He |e author |
| 700 | 1 | 0 | |a Xue Teng |e author |
| 700 | 1 | 0 | |a Jing Mi |e author |
| 700 | 1 | 0 | |a Jing Yang |e author |
| 700 | 1 | 0 | |a Rongrui Wei |e author |
| 700 | 1 | 0 | |a Wenmin Liu |e author |
| 700 | 1 | 0 | |a Qinge Ma |e author |
| 700 | 1 | 0 | |a Zhenghuai Tan |e author |
| 700 | 1 | 0 | |a Zhipei Sang |e author |
| 245 | 0 | 0 | |a Development of novel salicylic acid-donepezil-rivastigmine hybrids as multifunctional agents for the treatment of Alzheimer's disease |
| 260 | |b Taylor & Francis Group, |c 2023-12-01T00:00:00Z. | ||
| 500 | |a 10.1080/14756366.2023.2231661 | ||
| 500 | |a 1475-6374 | ||
| 500 | |a 1475-6366 | ||
| 520 | |a Alzheimer's disease (AD) is a chronic, progressive brain degenerative disease that is common in the elderly. So far, there is no effective treatment. The multi-target-directed ligands (MTDLs) strategy has been recognised as the most promising approach due to the complexity of the pathogenesis of AD. Herein, novel salicylic acid-donepezil-rivastigmine hybrids were designed and synthesised. The bioactivity results exhibited that 5a was a reversible and selective eqBChE inhibitor (IC50 = 0.53 μM), and the docking provided the possible mechanism. Compound 5a also displayed potential anti-inflammatory effects and significant neuroprotective effect. Moreover, 5a exhibited favourable stabilities in artificial gastrointestinal solution and plasma. Finally, 5a demonstrated potential cognitive improvement in scopolamine-induced cognitive dysfunction. Hence, 5a was a potential multifunctional lead compound against AD. | ||
| 546 | |a EN | ||
| 690 | |a Alzheimer's disease | ||
| 690 | |a salicylic acid-donepezil-rivastigmine hybrids | ||
| 690 | |a multi-functional agent | ||
| 690 | |a drug-likeness | ||
| 690 | |a scopolamine-induced AD model | ||
| 690 | |a Therapeutics. Pharmacology | ||
| 690 | |a RM1-950 | ||
| 655 | 7 | |a article |2 local | |
| 786 | 0 | |n Journal of Enzyme Inhibition and Medicinal Chemistry, Vol 38, Iss 1 (2023) | |
| 787 | 0 | |n https://www.tandfonline.com/doi/10.1080/14756366.2023.2231661 | |
| 787 | 0 | |n https://doaj.org/toc/1475-6366 | |
| 787 | 0 | |n https://doaj.org/toc/1475-6374 | |
| 856 | 4 | 1 | |u https://doaj.org/article/01e902f90d2041f1bf78b8a7c5596af2 |z Connect to this object online. |