Please use this identifier to cite or link to this item:
https://hdl.handle.net/10316/107437
DC Field | Value | Language |
---|---|---|
dc.contributor.author | Alves, Nuno Guerreiro | - |
dc.contributor.author | Bártolo, Inês | - |
dc.contributor.author | Alves, Américo J. S. | - |
dc.contributor.author | Fontinha, Diana | - |
dc.contributor.author | Francisco, Denise | - |
dc.contributor.author | Lopes, Susana M. M. | - |
dc.contributor.author | Soares, Maria I. L. | - |
dc.contributor.author | Simões, Carlos J. V. | - |
dc.contributor.author | Prudêncio, Miguel | - |
dc.contributor.author | Taveira, Nuno | - |
dc.contributor.author | Pinho e Melo, Teresa M. V. D. | - |
dc.date.accessioned | 2023-07-12T08:21:03Z | - |
dc.date.available | 2023-07-12T08:21:03Z | - |
dc.date.issued | 2021-07-05 | - |
dc.identifier.issn | 02235234 | pt |
dc.identifier.uri | https://hdl.handle.net/10316/107437 | - |
dc.description.abstract | The synthesis and antimicrobial activity of new spiro-β-lactams is reported. The design of the new molecules was based on the structural modulation of two previously identified lead spiro-penicillanates with dual activity against HIV and Plasmodium. The spiro-β-lactams synthesized were assayed for their in vitro activity against HIV-1, providing relevant structure-activity relationship information. Among the tested compounds, two spirocyclopentenyl-β-lactams were identified as having remarkable nanomolar activity against HIV-1. Additionally, the same molecules showed promising antiplasmodial activity, inhibiting both the hepatic and blood stages of Plasmodium infection. | pt |
dc.language.iso | eng | pt |
dc.publisher | Elsevier | pt |
dc.relation | SFRH/BD/128910/2017 | pt |
dc.relation | PD/BD/135287/2017 | pt |
dc.relation | UIDB/04138/2020 | pt |
dc.relation | UIDB/00313/2020 | pt |
dc.relation | UIDP/00313/2020 | pt |
dc.rights | embargoedAccess | pt |
dc.rights.uri | http://creativecommons.org/licenses/by-nc-nd/4.0/ | pt |
dc.subject | 1,3-Dipolar cycloaddition | pt |
dc.subject | 2-Butynoates | pt |
dc.subject | Allenes | pt |
dc.subject | Anti-HIV agents | pt |
dc.subject | Antiplasmodial agents | pt |
dc.subject | Phosphane-catalyzed [3+2] annulations | pt |
dc.subject | Spiro-3H-pyrazole-β-lactams | pt |
dc.subject | Spiro-penicillanates | pt |
dc.subject | Spirocyclic compounds | pt |
dc.subject | Spirocyclopentenyl-β-lactams; β-Lactams | pt |
dc.subject.mesh | Anti-HIV Agents | pt |
dc.subject.mesh | Antimalarials | pt |
dc.subject.mesh | Cell Line | pt |
dc.subject.mesh | Cell Survival | pt |
dc.subject.mesh | Drug Design | pt |
dc.subject.mesh | HIV-1 | pt |
dc.subject.mesh | Humans | pt |
dc.subject.mesh | Life Cycle Stages | pt |
dc.subject.mesh | Molecular Conformation | pt |
dc.subject.mesh | Plasmodium | pt |
dc.subject.mesh | Spiro Compounds | pt |
dc.subject.mesh | Stereoisomerism | pt |
dc.subject.mesh | Structure-Activity Relationship | pt |
dc.subject.mesh | beta-Lactams | pt |
dc.title | Synthesis and structure-activity relationships of new chiral spiro-β-lactams highly active against HIV-1 and Plasmodium | pt |
dc.type | article | - |
degois.publication.firstPage | 113439 | pt |
degois.publication.title | European Journal of Medicinal Chemistry | pt |
dc.peerreviewed | yes | pt |
dc.identifier.doi | 10.1016/j.ejmech.2021.113439 | pt |
degois.publication.volume | 219 | pt |
dc.date.embargo | 2023-07-05 | * |
uc.date.periodoEmbargo | 730 | pt |
item.openairecristype | http://purl.org/coar/resource_type/c_18cf | - |
item.grantfulltext | open | - |
item.openairetype | article | - |
item.languageiso639-1 | en | - |
item.fulltext | Com Texto completo | - |
item.cerifentitytype | Publications | - |
crisitem.project.grantno | Research Institute for Medicines - iMed.ULisboa | - |
crisitem.project.grantno | Coimbra Chemistry Center | - |
crisitem.project.grantno | Coimbra Chemistry Center | - |
crisitem.author.researchunit | CQC - Coimbra Chemistry Centre | - |
crisitem.author.researchunit | CQC - Coimbra Chemistry Centre | - |
crisitem.author.researchunit | CQC - Coimbra Chemistry Centre | - |
crisitem.author.researchunit | CQC - Coimbra Chemistry Centre | - |
crisitem.author.researchunit | CQC - Coimbra Chemistry Centre | - |
crisitem.author.parentresearchunit | Faculty of Sciences and Technology | - |
crisitem.author.parentresearchunit | Faculty of Sciences and Technology | - |
crisitem.author.parentresearchunit | Faculty of Sciences and Technology | - |
crisitem.author.parentresearchunit | Faculty of Sciences and Technology | - |
crisitem.author.parentresearchunit | Faculty of Sciences and Technology | - |
crisitem.author.orcid | 0000-0001-8860-0470 | - |
crisitem.author.orcid | 0000-0001-5994-9104 | - |
crisitem.author.orcid | 0000-0003-3256-4954 | - |
Appears in Collections: | I&D CQC - Artigos em Revistas Internacionais |
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File | Description | Size | Format | |
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Alves2021EurJMedChem.pdf | 2.38 MB | Adobe PDF | View/Open |
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