Structural Modifications on Chalcone Framework for Developing New Class of Cholinesterase Inhibitors
Due to the multifaceted pharmacological activities of chalcones, these scaffolds have been considered one of the most privileged frameworks in the drug discovery process. Structurally, chalcones are α, β-unsaturated carbonyl functionalities with two aryl or heteroaryl units. Amongst the numerous pha...
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MDPI AG
2022-03-01
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| Series: | International Journal of Molecular Sciences |
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| Online Access: | https://www.mdpi.com/1422-0067/23/6/3121 |
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| author | Ginson George Vishal Payyalot Koyiparambath Sunitha Sukumaran Aathira Sujathan Nair Leena K. Pappachan Abdullah G. Al-Sehemi Hoon Kim Bijo Mathew |
| author_facet | Ginson George Vishal Payyalot Koyiparambath Sunitha Sukumaran Aathira Sujathan Nair Leena K. Pappachan Abdullah G. Al-Sehemi Hoon Kim Bijo Mathew |
| author_sort | Ginson George |
| collection | DOAJ |
| description | Due to the multifaceted pharmacological activities of chalcones, these scaffolds have been considered one of the most privileged frameworks in the drug discovery process. Structurally, chalcones are α, β-unsaturated carbonyl functionalities with two aryl or heteroaryl units. Amongst the numerous pharmacological activities explored for chalcone derivatives, the development of novel chalcone analogs for the treatment of Alzheimer’s disease (AD) is among the research topics of most interest. Chalcones possess numerous advantages, such as smaller molecular size, opportunities for further structural modification thereby altering the physicochemical properties, cost-effectiveness, and convenient synthetic methodology. The present review highlights the recent evidence of chalcones as a privileged structure in AD drug development processes. Different classes of chalcone-derived analogs are summarized for the easy understanding of the previously reported analogs as well as the importance of certain functionalities in exhibiting cholinesterase inhibition. In this way, this review will shed light on the medicinal chemistry fraternity for the design and development of novel promising chalcone candidates for the treatment of AD. |
| first_indexed | 2024-03-09T19:42:39Z |
| format | Article |
| id | doaj.art-a7fca4d9642442ccb9f744f2b64c88b4 |
| institution | Directory Open Access Journal |
| issn | 1661-6596 1422-0067 |
| language | English |
| last_indexed | 2024-03-09T19:42:39Z |
| publishDate | 2022-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | International Journal of Molecular Sciences |
| spelling | doaj.art-a7fca4d9642442ccb9f744f2b64c88b42023-11-24T01:32:55ZengMDPI AGInternational Journal of Molecular Sciences1661-65961422-00672022-03-01236312110.3390/ijms23063121Structural Modifications on Chalcone Framework for Developing New Class of Cholinesterase InhibitorsGinson George0Vishal Payyalot Koyiparambath1Sunitha Sukumaran2Aathira Sujathan Nair3Leena K. Pappachan4Abdullah G. Al-Sehemi5Hoon Kim6Bijo Mathew7Department of Pharmaceutical Chemistry, Amrita School of Pharmacy, AIMS Health Sciences Campus, Amrita Vishwa Vidyapeetham, Kochi 682 041, IndiaDepartment of Pharmaceutical Chemistry, Amrita School of Pharmacy, AIMS Health Sciences Campus, Amrita Vishwa Vidyapeetham, Kochi 682 041, IndiaDepartment of Pharmaceutical Chemistry, Amrita School of Pharmacy, AIMS Health Sciences Campus, Amrita Vishwa Vidyapeetham, Kochi 682 041, IndiaDepartment of Pharmaceutical Chemistry, Amrita School of Pharmacy, AIMS Health Sciences Campus, Amrita Vishwa Vidyapeetham, Kochi 682 041, IndiaDepartment of Pharmaceutical Chemistry, Amrita School of Pharmacy, AIMS Health Sciences Campus, Amrita Vishwa Vidyapeetham, Kochi 682 041, IndiaResearch Center for Advanced Materials Science (RCAMS), King Khalid University, P.O. Box 9004, Abha 61413, Saudi ArabiaDepartment of Pharmacy, Sunchon National University, Suncheon 57922, KoreaDepartment of Pharmaceutical Chemistry, Amrita School of Pharmacy, AIMS Health Sciences Campus, Amrita Vishwa Vidyapeetham, Kochi 682 041, IndiaDue to the multifaceted pharmacological activities of chalcones, these scaffolds have been considered one of the most privileged frameworks in the drug discovery process. Structurally, chalcones are α, β-unsaturated carbonyl functionalities with two aryl or heteroaryl units. Amongst the numerous pharmacological activities explored for chalcone derivatives, the development of novel chalcone analogs for the treatment of Alzheimer’s disease (AD) is among the research topics of most interest. Chalcones possess numerous advantages, such as smaller molecular size, opportunities for further structural modification thereby altering the physicochemical properties, cost-effectiveness, and convenient synthetic methodology. The present review highlights the recent evidence of chalcones as a privileged structure in AD drug development processes. Different classes of chalcone-derived analogs are summarized for the easy understanding of the previously reported analogs as well as the importance of certain functionalities in exhibiting cholinesterase inhibition. In this way, this review will shed light on the medicinal chemistry fraternity for the design and development of novel promising chalcone candidates for the treatment of AD.https://www.mdpi.com/1422-0067/23/6/3121chalconesacetylcholinesterasebutyrylcholinesterasestructure activity relationships |
| spellingShingle | Ginson George Vishal Payyalot Koyiparambath Sunitha Sukumaran Aathira Sujathan Nair Leena K. Pappachan Abdullah G. Al-Sehemi Hoon Kim Bijo Mathew Structural Modifications on Chalcone Framework for Developing New Class of Cholinesterase Inhibitors International Journal of Molecular Sciences chalcones acetylcholinesterase butyrylcholinesterase structure activity relationships |
| title | Structural Modifications on Chalcone Framework for Developing New Class of Cholinesterase Inhibitors |
| title_full | Structural Modifications on Chalcone Framework for Developing New Class of Cholinesterase Inhibitors |
| title_fullStr | Structural Modifications on Chalcone Framework for Developing New Class of Cholinesterase Inhibitors |
| title_full_unstemmed | Structural Modifications on Chalcone Framework for Developing New Class of Cholinesterase Inhibitors |
| title_short | Structural Modifications on Chalcone Framework for Developing New Class of Cholinesterase Inhibitors |
| title_sort | structural modifications on chalcone framework for developing new class of cholinesterase inhibitors |
| topic | chalcones acetylcholinesterase butyrylcholinesterase structure activity relationships |
| url | https://www.mdpi.com/1422-0067/23/6/3121 |
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