Synthesis and evaluation of benzothiazole-triazole and benzothiadiazole-triazole scaffolds as potential molecular probes for amyloid-β aggregation

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dc.creatorChristine Dyrager
dc.creatorRafael Pinto Vieira
dc.creatorSofie Nyström
dc.creatorK. Peter R. Nilsson
dc.creatorTim Storr
dc.date.accessioned2023-07-14T20:05:03Z
dc.date.accessioned2025-09-09T00:19:34Z
dc.date.available2023-07-14T20:05:03Z
dc.date.issued2017
dc.description.sponsorshipCNPq - Conselho Nacional de Desenvolvimento Científico e Tecnológico
dc.description.sponsorshipCAPES - Coordenação de Aperfeiçoamento de Pessoal de Nível Superior
dc.format.mimetypepdf
dc.identifier.doihttps://doi.org/10.1039/C6NJ01703G
dc.identifier.issn1369-9261
dc.identifier.urihttps://hdl.handle.net/1843/56274
dc.languageeng
dc.publisherUniversidade Federal de Minas Gerais
dc.relation.ispartofNew Journal of Chemistry
dc.rightsAcesso Restrito
dc.subjectFungicidas
dc.subjectDoença de Alzheimer
dc.subjectDoenças neurodegenerativas
dc.subject.otherBenzothiazole-triazole
dc.subject.otherAlzheimer’s disease
dc.subject.otherNeurodegenerative disorders
dc.titleSynthesis and evaluation of benzothiazole-triazole and benzothiadiazole-triazole scaffolds as potential molecular probes for amyloid-β aggregation
dc.typeArtigo de periódico
local.citation.epage1573
local.citation.spage1566
local.citation.volume41
local.description.resumoSmall-molecule ligands that bind to misfolded protein aggregates are essential tools for the study and detection of pathological hallmarks in neurodegenerative disorders, such as Alzheimer's disease (AD). In the present study, three compounds (one benzothiazole-triazole, L1, and two benzothiadiazole-triazoles, L2 and L3) were synthesized via a modular approach (azide–alkyne cycloaddition) and evaluated as potential ligands for amyloid-β (Aβ) aggregates. The binding to amyloid-like fibrils, generated from recombinant Aβ1–42, were studied and the binding specificity to amyloid deposits was evaluated in brain sections from transgenic mice with AD pathology. All three derivatives showed significant reduced emission in the presence of recombinant Aβ1–42 amyloid fibrils. In addition, the observed binding to Aβ deposits in tissue sections suggests that the benzothiazole-triazole and benzothiadiazole-triazole structures are promising molecular scaffolds that can be modified for binding to specific protein aggregates.
local.identifier.orcidhttps://orcid.org/0000-0003-4647-9769
local.identifier.orcidhttps://orcid.org/0000-0003-3176-1681
local.publisher.countryBrasil
local.publisher.departmentICB - DEPARTAMENTO DE BIOQUÍMICA E IMUNOLOGIA
local.publisher.initialsUFMG
local.url.externahttps://pubs.rsc.org/en/content/articlelanding/2017/NJ/C6NJ01703G

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