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Metadados | Descrição | Idioma |
---|---|---|
Autor(es): dc.contributor | University of Vienna | - |
Autor(es): dc.contributor | Ural Federal University Named after the First President of Russia B. N. Yeltsin | - |
Autor(es): dc.contributor | Medical University of Vienna | - |
Autor(es): dc.contributor | Universidade de São Paulo (USP) | - |
Autor(es): dc.contributor | Paracelsus Medical University | - |
Autor(es): dc.creator | Kalaba, Predrag | - |
Autor(es): dc.creator | Aher, Nilima Y. | - |
Autor(es): dc.creator | Ilić, Marija | - |
Autor(es): dc.creator | Dragačević, Vladimir | - |
Autor(es): dc.creator | Wieder, Marcus | - |
Autor(es): dc.creator | Miklosi, Andras G. | - |
Autor(es): dc.creator | Zehl, Martin | - |
Autor(es): dc.creator | Wackerlig, Judith | - |
Autor(es): dc.creator | Roller, Alexander | - |
Autor(es): dc.creator | Beryozkina, Tetyana | - |
Autor(es): dc.creator | Radoman, Bojana | - |
Autor(es): dc.creator | Saroja, Sivaprakasam R. | - |
Autor(es): dc.creator | Lindner, Wolfgang | - |
Autor(es): dc.creator | Gonzalez, Eduardo Perez | - |
Autor(es): dc.creator | Bakulev, Vasiliy | - |
Autor(es): dc.creator | Leban, Johann Jakob | - |
Autor(es): dc.creator | Sitte, Harald H. | - |
Autor(es): dc.creator | Urban, Ernst | - |
Autor(es): dc.creator | Langer, Thierry | - |
Autor(es): dc.creator | Lubec, Gert | - |
Data de aceite: dc.date.accessioned | 2022-08-04T22:06:49Z | - |
Data de disponibilização: dc.date.available | 2022-08-04T22:06:49Z | - |
Data de envio: dc.date.issued | 2022-04-28 | - |
Data de envio: dc.date.issued | 2022-04-28 | - |
Data de envio: dc.date.issued | 2017-11-22 | - |
Fonte completa do material: dc.identifier | http://dx.doi.org/10.1021/acs.jmedchem.7b01313 | - |
Fonte completa do material: dc.identifier | http://hdl.handle.net/11449/220967 | - |
Fonte: dc.identifier.uri | http://educapes.capes.gov.br/handle/11449/220967 | - |
Descrição: dc.description | Modafinil 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.description | Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) | - |
Descrição: dc.description | Department of Pharmaceutical Chemistry Faculty of Life Sciences University of Vienna, Althanstraße 14 | - |
Descrição: dc.description | Ural Federal University Named after the First President of Russia B. N. Yeltsin, 19 Mira St. | - |
Descrição: dc.description | Department of Analytical Chemistry Faculty of Chemistry University of Vienna, Währinger Straße 38 | - |
Descrição: dc.description | X-ray Structure Analysis Centre Faculty of Chemistry University of Vienna, Währinger Straße 38 | - |
Descrição: dc.description | Department of Pediatrics Medical University of Vienna | - |
Descrição: dc.description | Laboratory of Fine Organic Chemistry Department of Chemistry and Biochemistry Faculty of Science and Technology University of Sao Paulo State, Roberto Simonsen 305 | - |
Descrição: dc.description | Institute of Pharmacology Centre of Physiology and Pharmacology Medical University of Vienna | - |
Descrição: dc.description | Neuroscience Laboratory Paracelsus Medical University | - |
Descrição: dc.description | FAPESP: 2016/10149-0 | - |
Formato: dc.format | 9330-9348 | - |
Idioma: dc.language | en | - |
Relação: dc.relation | Journal of Medicinal Chemistry | - |
???dc.source???: dc.source | Scopus | - |
Título: dc.title | Heterocyclic Analogues of Modafinil as Novel, Atypical Dopamine Transporter Inhibitors | - |
Tipo de arquivo: dc.type | livro digital | - |
Aparece nas coleções: | Repositório Institucional - Unesp |
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