Synthesis and dopamine receptor binding of dihydrexidine and SKF 38393 catecholamine-based analogues

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Autor(es): dc.contributorUniversidade Estadual Paulista (UNESP)-
Autor(es): dc.contributorUniversity of Vienna-
Autor(es): dc.contributorUniversidade de São Paulo (USP)-
Autor(es): dc.contributorMedical University of Vienna-
Autor(es): dc.contributorParacelsus Medical University-
Autor(es): dc.creatorda Silva, Suzane Rosa-
Autor(es): dc.creatorKalaba, Predrag-
Autor(es): dc.creatorFabišiková, Anna-
Autor(es): dc.creatorZehl, Martin-
Autor(es): dc.creatorDragačević, Vladimir-
Autor(es): dc.creatordos Anjos, Luana Ribeiro-
Autor(es): dc.creatorNeill, Philip John-
Autor(es): dc.creatorWieder, Marcus-
Autor(es): dc.creatorPrado-Roller, Alexander-
Autor(es): dc.creatorGajic, Natalie-
Autor(es): dc.creatorPalaretti, Vinicius-
Autor(es): dc.creatorda Silva, Gil Valdo Jose-
Autor(es): dc.creatorPifl, Christian-
Autor(es): dc.creatorLubec, Gert-
Autor(es): dc.creatorGonzalez, Eduardo R. Perez-
Data de aceite: dc.date.accessioned2025-08-21T16:29:22Z-
Data de disponibilização: dc.date.available2025-08-21T16:29:22Z-
Data de envio: dc.date.issued2022-04-28-
Data de envio: dc.date.issued2022-04-28-
Data de envio: dc.date.issued2021-12-31-
Fonte completa do material: dc.identifierhttp://dx.doi.org/10.1007/s00726-021-03106-4-
Fonte completa do material: dc.identifierhttp://hdl.handle.net/11449/222946-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/222946-
Descrição: dc.descriptionDopamine is an important neurotransmitter that regulates numerous essential functions, including cognition and voluntary movement. As such, it serves as an important scaffold for synthesis of novel analogues as part of drug development effort to obtain drugs for treatment of neurodegenerative diseases, such as Parkinson's disease. To that end, similarity search of the ZINC database based on two known dopamine-1 receptor (D1R) agonists, dihydrexidine (DHX) and SKF 38393, respectively, was used to predict novel chemical entities with potential binding to D1R. Three compounds that showed the highest similarity index were selected for synthesis and bioactivity profiling. All main synthesis products as well as the isolated intermediates, were properly characterized. The physico-chemical analyses were performed using HRESIMS, GC/MS, LC/MS with UV–Vis detection, and FTIR, 1H NMR and 13C NMR spectroscopy. Binding to D1 and D2 receptors and inhibition of dopamine reuptake via dopamine transporter were measured for the synthesized analogues of DHX and SKF 38393.-
Descrição: dc.descriptionFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)-
Descrição: dc.descriptionLaboratory of Fine Organic Chemistry Department of Chemistry and Biochemistry Faculty of Sciences and Technology of São Paulo State University, São Paulo-
Descrição: dc.descriptionDepartment of Pharmaceutical Chemistry Faculty of Life Sciences University of Vienna, Althanstraße 14-
Descrição: dc.descriptionMass Spectrometry Centre Faculty of Chemistry University of Vienna, Währinger Straße 38-
Descrição: dc.descriptionDepartment of Analytical Chemistry Faculty of Chemistry University of Vienna, Währinger Straße 38-
Descrição: dc.descriptionCentre for X-Ray Structure Analysis at Faculty of Chemistry University of Vienna, Währinger Straße 40-42-
Descrição: dc.descriptionDepartment of Chemistry Faculty of Philosophy Sciences and Letters of Ribeirão Preto University of São Paulo, Avenida dos Bandeirantes, 3900, SP-
Descrição: dc.descriptionDepartment of Molecular Neurosciences Centre for Brain Research Medical University of Vienna, Spitalgasse 4-
Descrição: dc.descriptionDepartment of Neuroproteomics Paracelsus Medical University-
Descrição: dc.descriptionLaboratory of Fine Organic Chemistry Department of Chemistry and Biochemistry Faculty of Sciences and Technology of São Paulo State University, São Paulo-
Descrição: dc.descriptionFAPESP: 2016/10149-0-
Formato: dc.format85-98-
Idioma: dc.languageen-
Relação: dc.relationAmino Acids-
???dc.source???: dc.sourceScopus-
Palavras-chave: dc.subjectD1R agonists-
Palavras-chave: dc.subjectD2R and DAT-
Palavras-chave: dc.subjectDihydrexidine-
Palavras-chave: dc.subjectDopamine analogs-
Palavras-chave: dc.subjectSKF 38393-
Título: dc.titleSynthesis and dopamine receptor binding of dihydrexidine and SKF 38393 catecholamine-based analogues-
Tipo de arquivo: dc.typelivro digital-
Aparece nas coleções:Repositório Institucional - Unesp

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