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https://hdl.handle.net/10316/107711
Título: | Donepezil structure-based hybrids as potential multifunctional anti-Alzheimer's drug candidates | Autor: | Piemontese, Luca Tomás, Daniel Hiremathad, Asha Capriati, Vito Candeias, Emanuel Cardoso, Sandra M. Chaves, Sílvia Santos, M. Amélia |
Palavras-chave: | Alzheimer’s disease; multipotent drugs; donepezil mimetics; AChE inhibitors; anti-Aβ aggregation | Data: | Dez-2018 | Editora: | Taylor & Francis | Projeto: | UID/QUI/00100/2013 PEst-C/SAU/LA0001/2011–2013 Fondo di Sviluppo e Coesione 2007–2013–APQ Ricerca Regione Puglia “Programma regionale a sostegno della specializzazione intelligente e della sostenibilit a sociale ed ambientale - Future In Research”. Project ID: I2PCTF6 |
Título da revista, periódico, livro ou evento: | Journal of Enzyme Inhibition and Medicinal Chemistry | Volume: | 33 | Número: | 1 | Resumo: | A new series of multifunctional hybrids, based on the structure of the donepezil (DNP) drug, have been developed and evaluated as potential anti Alzheimer's disease (AD) agents. The rationale of this study was the conjugation of a benzylpiperidine/benzylpiperazine moiety with derivatives of bioactive heterocyclics (benzimidazole or benzofuran), to mimic the main structure of DNP and to endow the hybrids with additional relevant properties such as inhibition of amyloid beta (Aβ) peptide aggregation, antioxidant activity and metal chelation. Overall, they showed good activity for AChE inhibition (IC50=4.0-30.0 μΜ) and moderate ability for inhibition of Aβ1-42 self-mediated aggregation. The hybrids containing chelating groups showed improvement in the inhibition of Cu-induced Aβ42 aggregation and the antioxidant capacity. Moreover, neuroprotective effects of these compounds were evidenced in neuroblastoma cells after Aβ1-42 induced toxicity. Structure-activity relationship allowed the identification of some promising compounds and the main determinant structural features for the targeted properties. | URI: | https://hdl.handle.net/10316/107711 | ISSN: | 1475-6366 1475-6374 |
DOI: | 10.1080/14756366.2018.1491564 | Direitos: | openAccess |
Aparece nas coleções: | FMUC Medicina - Artigos em Revistas Internacionais I&D CNC - Artigos em Revistas Internacionais |
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Donepezil-structurebased-hybrids-as-potential-multifunctional-antiAlzheimers-drug-candidatesJournal-of-Enzyme-Inhibition-and-Medicinal-Chemistry.pdf | 3.69 MB | Adobe PDF | Ver/Abrir |
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