Please use this identifier to cite or link to this item:
https://hdl.handle.net/10316/25285
DC Field | Value | Language |
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dc.contributor.author | Rucins, Martins | - |
dc.contributor.author | Kaldre, Dainis | - |
dc.contributor.author | Pajuste, Karlis | - |
dc.contributor.author | Fernandes, Maria A. S. | - |
dc.contributor.author | Vicente, Joaquim A. F. | - |
dc.contributor.author | Klimaviciusa, Linda | - |
dc.contributor.author | Jaschenko, Elina | - |
dc.contributor.author | Kanepe-Lapsa, Iveta | - |
dc.contributor.author | Shestakova, Irina | - |
dc.contributor.author | Plotniece, Mara | - |
dc.contributor.author | Gosteva, Marina | - |
dc.contributor.author | Sobolev, Arkadij | - |
dc.contributor.author | Jansone, Baiba | - |
dc.contributor.author | Muceniece, Ruta | - |
dc.contributor.author | Klusa, Vija | - |
dc.contributor.author | Plotniece, Aiva | - |
dc.date.accessioned | 2014-02-28T11:56:05Z | - |
dc.date.available | 2014-02-28T11:56:05Z | - |
dc.date.issued | 2014 | - |
dc.identifier.issn | 1631-0748 | - |
dc.identifier.uri | https://hdl.handle.net/10316/25285 | - |
dc.description.abstract | The novel 1,4-dihydropyridine derivatives containing the cationic pyridine moiety at the position 4, and the N-propargyl group as a substituent at position 1 of the 1,4-DHP cycle were designed, synthesised, and assessed in biological tests. Among all the novel compounds, the 4-(N-dodecyl) pyridinium group-containing compounds 11 (without the N-propargyl group) and 12 (with the N-propargyl group) demonstrated the highest calcium antagonistic properties against neuroblastoma SH-SY5Y (IC50 about 5–14 mM) and the vascular smooth muscle A7r5 cell (IC50 – 0.6–0.7 mM) lines, indicating that they predominantly target the L-type calcium channels. These compounds showed a slight total antioxidant activity. At concentrations close to those of L-type calcium channel blocking ones, compound 12 did not affect mitochondrial functioning; also, no toxicity was obtained in vivo. The N-propargyl group as a substituent at position 1 of the 1,4-DHP cycle did not essentially influence the compounds’ activity. The 4-(N-dodecyl) pyridinium moiety-containing compounds can be considered as prototype molecules for further chemical modifications and studies as cardioprotective/neuroprotective agents. | por |
dc.description.sponsorship | This study was supported by ESF project No. 2009/ 0217/1DP/1.1.1.2.0/09/APIA/VIAA/031; the EuroNanoMed project ‘‘CheTherDel’’; Portuguese Research Council (FCT), Faculty of Medicine, Centre for Neuroscience and Cell Biology (CNC) and Marine and Environmental Research Centre (IMAR–CMA) of the University of Coimbra, Portugal. | por |
dc.language.iso | eng | por |
dc.publisher | Académie des sciences | por |
dc.rights | openAccess | por |
dc.subject | 1,4-Dihydropyridines | por |
dc.subject | N-Dodecyl pyridinium | por |
dc.subject | Propargyl substituent | por |
dc.subject | Calcium antagonists | por |
dc.subject | Antioxidant activity | por |
dc.subject | Mitochondrial processes | por |
dc.subject | Structure–activity relationships | por |
dc.title | Synthesis and studies of calcium channel blocking and antioxidant activities of novel 4-pyridinium and/or N-propargyl substituted 1,4-dihydropyridine derivatives | por |
dc.type | article | por |
degois.publication.firstPage | 69 | por |
degois.publication.lastPage | 80 | por |
degois.publication.issue | 1 | por |
degois.publication.title | Comptes Rendus Chimie | por |
dc.relation.publisherversion | http://www.sciencedirect.com/science/article/pii/S1631074813002294# | por |
dc.peerreviewed | Yes | por |
dc.identifier.doi | 10.1016/j.crci.2013.07.003 | - |
degois.publication.volume | 17 | por |
item.fulltext | Com Texto completo | - |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.languageiso639-1 | en | - |
item.openairetype | article | - |
item.cerifentitytype | Publications | - |
item.grantfulltext | open | - |
Appears in Collections: | FCTUC Ciências da Vida - Artigos em Revistas Internacionais |
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1-s2.0-S1631074813002294-main.pdf | 729.7 kB | Adobe PDF | View/Open |
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