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Development of coumarin-benzofuran hybrids as versatile multitargeted compounds for the treatment of Alzheimer's Disease
Umeå University, Faculty of Science and Technology, Department of Chemistry.
2018 (English)In: Chemical Biology and Drug Design, ISSN 1747-0277, E-ISSN 1747-0285, Vol. 92, no 2, p. 1497-1503Article in journal (Refereed) Published
Abstract [en]

Alzheimer's disease (AD), the most common cause of dementia, is a neurodegenerative disorder characterized by progressive deterioration of memory and cognition. The evidenced multifactorial nature of AD has been considered the main reason for the absence of cure so far. Therefore, the development of novel hybrids to treat the disease is very much essential. Focusing on this, a novel series of coumarin-benzofuran hybrids have been designed and screened as anti-Alzheimer's disease agents. The strategy is to obtain an effective mimetic of donepezil, which is acetylcholinesterase inhibitor. Herein, the two main scaffolds namely coumarin and benzofuran are known pharmacophore moieties and we have performed their molecular design, pharmacokinetic descriptor studies for drug-likeliness. Further, in vitro studies such as antioxidant capacity, acetylcholinesterase (AChE) inhibition and amyloid-beta (A beta) self-aggregation inhibition have also been performed. Most importantly, these studies revealed that the newly synthesized hybrids can be versatile and promising drug-like moieties as efficient anti-AD agents.

Place, publisher, year, edition, pages
John Wiley & Sons, 2018. Vol. 92, no 2, p. 1497-1503
Keywords [en]
acetylcholinesterase inhibitors, Alzheimer's disease, benzofuran, coumarin
National Category
Pharmacology and Toxicology
Identifiers
URN: urn:nbn:se:umu:diva-150646DOI: 10.1111/cbdd.13316ISI: 000439752200011PubMedID: 29679445Scopus ID: 2-s2.0-85050492673OAI: oai:DiVA.org:umu-150646DiVA, id: diva2:1242790
Available from: 2018-08-29 Created: 2018-08-29 Last updated: 2018-08-29Bibliographically approved

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Chand, Karam

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CiteExportLink to record
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Citation style
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