Show simple item record

Development of Novel Potential Pleiotropic Compounds of Interest in Alzheimer’s Disease Treatment through Rigidification Strategy

dc.contributor.authorCédric Lecoutey
dc.contributor.authorRémi Legay
dc.contributor.authorAudrey Davis
dc.contributor.authorJana Sopková-de Oliveira Santos
dc.contributor.authorPatrick Dallemagne
dc.contributor.authorChristophe Rochais
dc.contributor.otherNormandie Univ, Unicaen, Cermn, 14000 Caen, France
dc.contributor.otherNormandie Univ, Unicaen, Cermn, 14000 Caen, France
dc.contributor.otherNormandie Univ, Unicaen, Cermn, 14000 Caen, France
dc.contributor.otherNormandie Univ, Unicaen, Cermn, 14000 Caen, France
dc.contributor.otherNormandie Univ, Unicaen, Cermn, 14000 Caen, France
dc.contributor.otherNormandie Univ, Unicaen, Cermn, 14000 Caen, France
dc.date.accessioned2021-04-27T00:05:21Z
dc.date.available2025-10-02T04:13:20Z
dc.date.issued01-04-2021
dc.identifier.issn-
dc.identifier.urihttps://www.mdpi.com/1420-3049/26/9/2536
dc.description.abstractThe development of Multi-Target Directed Ligand is of clear interest for the treatment of multifactorial pathology such as Alzheimer’s disease (AD). In this context, acetylcholinesterase (AChE) inhibitors have been modulated in order to generate novel pleiotropic compounds targeting a second protein of therapeutic interest in AD. Among them, donecopride was the first example of a dual acetylcholinesterase inhibitor and 5-HT<sub>4</sub> receptor agonist. In order to explore the structural diversity around this preclinical candidate we have explored the preparation of novel constrained analogs through late-stage rigidification strategy. A series of phenylpyrazoles was prepared in a late-stage functionalization process and all compounds were evaluated in vitro towards AChE and 5-HTRs. A docking study was performed in order to better explain the observed SAR towards AChE, 5-HT<sub>4</sub>R and 5-HT<sub>6</sub>R and this study led to the description of novel ligand targeting both AChE and 5-HT<sub>6</sub>R.
dc.format-
dc.language.isoEN
dc.publisherMDPI AG
dc.relation.uri['https://www.sciencedirect.com/journal/the-asian-journal-of-shipping-and-logistics', 'https://www.sciencedirect.com/journal/the-asian-journal-of-shipping-and-logistics/publish/guide-for-authors', 'https://www.elsevier.com/authors/open-access/choice#waivers']
dc.rights['CC BY', 'CC BY-NC-ND']
dc.subject['management', 'finance', 'accounting', 'insurance', 'international business', 'shipping', 'Shipment of goods. Delivery of goods', 'HF5761-5780']
dc.subject.lccOrganic chemistry
dc.titleDevelopment of Novel Potential Pleiotropic Compounds of Interest in Alzheimer’s Disease Treatment through Rigidification Strategy
dc.typeArticle
dc.description.keywordsAlzheimer’s disease
dc.description.keywordsacetylcholinesterase
dc.description.keywords5-HT<sub>6</sub>R
dc.description.keywordsdonecopride
dc.description.keywordsMTDL
dc.description.pages-
dc.description.doi10.3390/molecules26092536
dc.title.journalMolecules
dc.identifier.e-issn1420-3049
dc.identifier.oaioai:doaj.org/journal:180fb54093e947fcb689ef8f5c6a5fc4
dc.journal.infoVolume 26, Issue 9


This item appears in the following Collection(s)

Show simple item record