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Please use this identifier to cite or link to this item: http://hdl.handle.net/1843/69757
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dc.creatorBruna Silva Terrapt_BR
dc.creatorAngelo de Fátimapt_BR
dc.creatorPedro Henrique Correa da Silvapt_BR
dc.creatorAnna Tramarinpt_BR
dc.creatorLucas Lopardi Francopt_BR
dc.creatorElaine Fontes Ferreira da Cunhapt_BR
dc.creatorFernando César de Macedo Júniorpt_BR
dc.creatorTeodorico de Castro Ramalhopt_BR
dc.creatorManuela Bartolinipt_BR
dc.creatorMaria Laura Bolognesipt_BR
dc.date.accessioned2024-07-05T17:17:45Z-
dc.date.available2024-07-05T17:17:45Z-
dc.date.issued2018-
dc.citation.volume29pt_BR
dc.citation.issue4pt_BR
dc.citation.spage738pt_BR
dc.citation.epage747pt_BR
dc.identifier.doihttp://dx.doi.org/10.21577/0103-5053.20170196pt_BR
dc.identifier.issn0103-5053pt_BR
dc.identifier.urihttp://hdl.handle.net/1843/69757-
dc.description.resumoAlzheimer disease (AD) is a complex disease related to multiple pathogenic mechanisms. A strategy to develop effective drugs is based on the so-called multi-target directed ligands (MTDL) by using hybrid compounds. So, in the present study, we have designed and synthesized two hybrids, containing the indanone-piperidine moiety of donepezil, a drug approved for the treatment of AD, and the lipoic acid scaffold, an antioxidant compound endowed with neuroprotective effects. One hybrid was synthesized in four steps with 42% global yield, and the other hybrid in six steps with 19% global yield. The latter hybrid displayed moderate inhibitory activity against human acetylcholinesterase (hAChE) and greater activity against human butyrylcholinesterases (hBuChE). The selectivity for hBuChE was further rationalized by theoretical study. Importantly, the second hybrid showed a good antioxidant activity, exhibiting better ability in scavenging 2,2-diphenyl 1-picrylhydrazyl (DPPH) radicals than lipoic acid.pt_BR
dc.description.sponsorshipCNPq - Conselho Nacional de Desenvolvimento Científico e Tecnológicopt_BR
dc.description.sponsorshipFAPEMIG - Fundação de Amparo à Pesquisa do Estado de Minas Geraispt_BR
dc.description.sponsorshipCAPES - Coordenação de Aperfeiçoamento de Pessoal de Nível Superiorpt_BR
dc.description.sponsorshipOutra Agênciapt_BR
dc.format.mimetypepdfpt_BR
dc.languageengpt_BR
dc.publisherUniversidade Federal de Minas Geraispt_BR
dc.publisher.countryBrasilpt_BR
dc.publisher.departmentICX - DEPARTAMENTO DE QUÍMICApt_BR
dc.publisher.initialsUFMGpt_BR
dc.relation.ispartofJournal of the Brazilian Chemical Society-
dc.rightsAcesso Abertopt_BR
dc.subjectDonepezil-lipoic acid hybridspt_BR
dc.subjectAlzheimer diseasept_BR
dc.subjectMulti-target directed ligandspt_BR
dc.subject.otherAntioxidantespt_BR
dc.subject.otherAlzheimer, Doença dept_BR
dc.subject.otherInibidores da colinesterasept_BR
dc.titleTwo novel donepezil-lipoic acid hybrids: synthesis, anticholinesterase and antioxidant activities and theoretical studiespt_BR
dc.typeArtigo de Periódicopt_BR
dc.url.externahttps://jbcs.sbq.org.br/default.asp?ed=265pt_BR
dc.identifier.orcidhttps://orcid.org/0000-0002-9608-1559pt_BR
dc.identifier.orcidhttps://orcid.org/0000-0003-2344-5590pt_BR
dc.identifier.orcidhttps://orcid.org/0000-0002-5196-9845pt_BR
dc.identifier.orcidhttps://orcid.org/0000-0002-3845-3801pt_BR
dc.identifier.orcidhttps://orcid.org/0000-0002-4230-1309pt_BR
dc.identifier.orcidhttps://orcid.org/0000-0002-7324-1353pt_BR
dc.identifier.orcidhttps://orcid.org/0000-0002-2890-3856pt_BR
dc.identifier.orcidhttps://orcid.org/0000-0002-1289-5361pt_BR
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