Regioselective pyrrolizidine bis-spirooxindoles as efficient anti-amyloidogenic agents.

Alzheimer's disease Amyloid-β Protein misfolding Raman spectroscopy Spirooxindole

Journal

European journal of medicinal chemistry
ISSN: 1768-3254
Titre abrégé: Eur J Med Chem
Pays: France
ID NLM: 0420510

Informations de publication

Date de publication:
05 Oct 2022
Historique:
received: 03 05 2022
revised: 13 06 2022
accepted: 21 06 2022
pubmed: 6 7 2022
medline: 17 8 2022
entrez: 5 7 2022
Statut: ppublish

Résumé

Here, we report a microwave-assisted, one-pot, three-component, 1,3-dipolar cycloaddition reaction to produce highly regioselective and stereoselective bis-spirooxindoles as potential inhibitors against amyloid-β fibrillation. Ease of synthesis, promising anti-amyloidogenic activity, low toxicity, and in vitro blood brain barrier permeability makes these compounds attractive therapeutic leads to treat Alzheimer's disease.

Identifiants

pubmed: 35785723
pii: S0223-5234(22)00468-8
doi: 10.1016/j.ejmech.2022.114566
pii:
doi:

Substances chimiques

Amyloid beta-Peptides 0

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

114566

Informations de copyright

Copyright © 2022 Elsevier Masson SAS. All rights reserved.

Auteurs

Nilamuni H de Silva (NH)

School of Science, STEM College, RMIT University, 124 La Trobe Street, Melbourne, VIC, 3001, Australia. Electronic address: nilamuni.desilva@rmit.edu.au.

Anthony Dahdah (A)

School of Science, STEM College, RMIT University, 124 La Trobe Street, Melbourne, VIC, 3001, Australia.

Ewan W Blanch (EW)

School of Science, STEM College, RMIT University, 124 La Trobe Street, Melbourne, VIC, 3001, Australia.

Helmut M Hügel (HM)

School of Science, STEM College, RMIT University, 124 La Trobe Street, Melbourne, VIC, 3001, Australia.

Subashani Maniam (S)

School of Science, STEM College, RMIT University, 124 La Trobe Street, Melbourne, VIC, 3001, Australia. Electronic address: subashani.maniam@rmit.edu.au.

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Classifications MeSH