Heterocyclic Analogues of Modafinil as Novel, Atypical Dopamine Transporter Inhibitors

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Autor(es): dc.contributorUniversity of Vienna-
Autor(es): dc.contributorUral Federal University Named after the First President of Russia B. N. Yeltsin-
Autor(es): dc.contributorMedical University of Vienna-
Autor(es): dc.contributorUniversidade de São Paulo (USP)-
Autor(es): dc.contributorParacelsus Medical University-
Autor(es): dc.creatorKalaba, Predrag-
Autor(es): dc.creatorAher, Nilima Y.-
Autor(es): dc.creatorIlić, Marija-
Autor(es): dc.creatorDragačević, Vladimir-
Autor(es): dc.creatorWieder, Marcus-
Autor(es): dc.creatorMiklosi, Andras G.-
Autor(es): dc.creatorZehl, Martin-
Autor(es): dc.creatorWackerlig, Judith-
Autor(es): dc.creatorRoller, Alexander-
Autor(es): dc.creatorBeryozkina, Tetyana-
Autor(es): dc.creatorRadoman, Bojana-
Autor(es): dc.creatorSaroja, Sivaprakasam R.-
Autor(es): dc.creatorLindner, Wolfgang-
Autor(es): dc.creatorGonzalez, Eduardo Perez-
Autor(es): dc.creatorBakulev, Vasiliy-
Autor(es): dc.creatorLeban, Johann Jakob-
Autor(es): dc.creatorSitte, Harald H.-
Autor(es): dc.creatorUrban, Ernst-
Autor(es): dc.creatorLanger, Thierry-
Autor(es): dc.creatorLubec, Gert-
Data de aceite: dc.date.accessioned2022-08-04T22:06:49Z-
Data de disponibilização: dc.date.available2022-08-04T22:06:49Z-
Data de envio: dc.date.issued2022-04-28-
Data de envio: dc.date.issued2022-04-28-
Data de envio: dc.date.issued2017-11-22-
Fonte completa do material: dc.identifierhttp://dx.doi.org/10.1021/acs.jmedchem.7b01313-
Fonte completa do material: dc.identifierhttp://hdl.handle.net/11449/220967-
Fonte: dc.identifier.urihttp://educapes.capes.gov.br/handle/11449/220967-
Descrição: dc.descriptionModafinil is a wake promoting compound with high potential for cognitive enhancement. It is targeting the dopamine transporter (DAT) with moderate selectivity, thereby leading to reuptake inhibition and increased dopamine levels in the synaptic cleft. A series of modafinil analogues have been reported so far, but more target-specific analogues remain to be discovered. It was the aim of this study to synthesize and characterize such analogues and, indeed, a series of compounds were showing higher activities on the DAT and a higher selectivity toward DAT versus serotonin and norepinephrine transporters than modafinil. This was achieved by substituting the amide moiety by five- and six-membered aromatic heterocycles. In vitro studies indicated binding to the cocaine pocket on DAT, although molecular dynamics revealed binding different from that of cocaine. Moreover, no release of dopamine was observed, ruling out amphetamine-like effects. The absence of neurotoxicity of a representative analogue may encourage further preclinical studies of the above-mentioned compounds.-
Descrição: dc.descriptionFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)-
Descrição: dc.descriptionDepartment of Pharmaceutical Chemistry Faculty of Life Sciences University of Vienna, Althanstraße 14-
Descrição: dc.descriptionUral Federal University Named after the First President of Russia B. N. Yeltsin, 19 Mira St.-
Descrição: dc.descriptionDepartment of Analytical Chemistry Faculty of Chemistry University of Vienna, Währinger Straße 38-
Descrição: dc.descriptionX-ray Structure Analysis Centre Faculty of Chemistry University of Vienna, Währinger Straße 38-
Descrição: dc.descriptionDepartment of Pediatrics Medical University of Vienna-
Descrição: dc.descriptionLaboratory of Fine Organic Chemistry Department of Chemistry and Biochemistry Faculty of Science and Technology University of Sao Paulo State, Roberto Simonsen 305-
Descrição: dc.descriptionInstitute of Pharmacology Centre of Physiology and Pharmacology Medical University of Vienna-
Descrição: dc.descriptionNeuroscience Laboratory Paracelsus Medical University-
Descrição: dc.descriptionFAPESP: 2016/10149-0-
Formato: dc.format9330-9348-
Idioma: dc.languageen-
Relação: dc.relationJournal of Medicinal Chemistry-
???dc.source???: dc.sourceScopus-
Título: dc.titleHeterocyclic Analogues of Modafinil as Novel, Atypical Dopamine Transporter Inhibitors-
Tipo de arquivo: dc.typelivro digital-
Aparece nas coleções:Repositório Institucional - Unesp

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