Design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part II)
A series of novel 4-isochromanone compounds bearing N-benzyl pyridinium moiety were designed and synthesized as acetylcholinesterase (AChE) inhibitors. The biological evaluation showed that most of the target compounds exhibited potent inhibitory activities against AChE. Among them, compound 1q poss...
| Main Authors: | , , , , , , , , |
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| Format: | Article |
| Language: | English |
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Wiley
2018
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| Online Access: | https://eprints.nottingham.ac.uk/47573/ |
| _version_ | 1848797579239751680 |
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| author | Wang, Jia Wang, Chaolei Wu, Zheng Li, Xinnan Xu, Shengtao Liu, Jie Lan, Qinying Zhu, Zheying Xu, Jinyi |
| author_facet | Wang, Jia Wang, Chaolei Wu, Zheng Li, Xinnan Xu, Shengtao Liu, Jie Lan, Qinying Zhu, Zheying Xu, Jinyi |
| author_sort | Wang, Jia |
| building | Nottingham Research Data Repository |
| collection | Online Access |
| description | A series of novel 4-isochromanone compounds bearing N-benzyl pyridinium moiety were designed and synthesized as acetylcholinesterase (AChE) inhibitors. The biological evaluation showed that most of the target compounds exhibited potent inhibitory activities against AChE. Among them, compound 1q possessed the strongest anti-AChE activity with an IC50 value of 0.15 nM and high AChE/BuChE selectivity (SI >5000). Moreover, compound 1q had low toxicity in normal nerve cells and was relatively stable in rat plasma. Together, the current finding may provide a new approach for the discovery of novel anti-Alzheimer’s disease agents. |
| first_indexed | 2025-11-14T20:06:07Z |
| format | Article |
| id | nottingham-47573 |
| institution | University of Nottingham Malaysia Campus |
| institution_category | Local University |
| language | English |
| last_indexed | 2025-11-14T20:06:07Z |
| publishDate | 2018 |
| publisher | Wiley |
| recordtype | eprints |
| repository_type | Digital Repository |
| spelling | nottingham-475732018-11-07T04:30:11Z https://eprints.nottingham.ac.uk/47573/ Design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part II) Wang, Jia Wang, Chaolei Wu, Zheng Li, Xinnan Xu, Shengtao Liu, Jie Lan, Qinying Zhu, Zheying Xu, Jinyi A series of novel 4-isochromanone compounds bearing N-benzyl pyridinium moiety were designed and synthesized as acetylcholinesterase (AChE) inhibitors. The biological evaluation showed that most of the target compounds exhibited potent inhibitory activities against AChE. Among them, compound 1q possessed the strongest anti-AChE activity with an IC50 value of 0.15 nM and high AChE/BuChE selectivity (SI >5000). Moreover, compound 1q had low toxicity in normal nerve cells and was relatively stable in rat plasma. Together, the current finding may provide a new approach for the discovery of novel anti-Alzheimer’s disease agents. Wiley 2018-02-21 Article PeerReviewed application/pdf en https://eprints.nottingham.ac.uk/47573/1/CBDD%202017-accepted.pdf Wang, Jia, Wang, Chaolei, Wu, Zheng, Li, Xinnan, Xu, Shengtao, Liu, Jie, Lan, Qinying, Zhu, Zheying and Xu, Jinyi (2018) Design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part II). Chemical Biology and Drug Design, 91 (3). pp. 756-762. ISSN 1747-0277 Alzheimer’s disease acetylcholinesterase inhibitors 4-isochromanone skeleton benzyl pyridine http://onlinelibrary.wiley.com/doi/10.1111/cbdd.13136/abstract doi:10.1111/cbdd.13136 doi:10.1111/cbdd.13136 |
| spellingShingle | Alzheimer’s disease acetylcholinesterase inhibitors 4-isochromanone skeleton benzyl pyridine Wang, Jia Wang, Chaolei Wu, Zheng Li, Xinnan Xu, Shengtao Liu, Jie Lan, Qinying Zhu, Zheying Xu, Jinyi Design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part II) |
| title | Design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part II) |
| title_full | Design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part II) |
| title_fullStr | Design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part II) |
| title_full_unstemmed | Design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part II) |
| title_short | Design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing N-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part II) |
| title_sort | design, synthesis, biological evaluation and docking study of 4-isochromanone hybrids bearing n-benzyl pyridinium moiety as dual binding site acetylcholinesterase inhibitors (part ii) |
| topic | Alzheimer’s disease acetylcholinesterase inhibitors 4-isochromanone skeleton benzyl pyridine |
| url | https://eprints.nottingham.ac.uk/47573/ https://eprints.nottingham.ac.uk/47573/ https://eprints.nottingham.ac.uk/47573/ |