The application of isatin-based multicomponent-reactions in the quest for new bioactive and druglike molecules
Autor(a) principal: | |
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Data de Publicação: | 2021 |
Outros Autores: | , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
Texto Completo: | http://hdl.handle.net/10316/93144 https://doi.org/10.1016/j.ejmech.2020.113102 |
Resumo: | Oxindole derivatives are known for their great interest in the field of Medicinal Chemistry, as they display vast biological activities. Recent efforts concerning the preparation of oxindole derivatives using isatin-based multicomponent reactions (MCRs) constitute a great advance in generating druglike libraries fast and with wide scaffold diversity. In this review, we address those recent developments, exploring the synthetic pathways and biological activities described for these compounds, namely antitumor, antibacterial, antifungal, antiparasitic, antiviral, antioxidant, anti-inflammatory and central nervous system (CNS) pathologies. To add new depth to this work, we used a well-established web-based free tool (SwissADME) to evaluate the most promising scaffolds in what concerns their druglike properties, namely by evaluating their compliance with some of the most valuable rules applied by medicinal chemists in both academia and industrial settings (Lipinski, Ghose, Veber, Egan, Muegge). The aim of this review is to endorse isatin-based MCRs as a valuable synthetic approach to attain new hit compounds bearing the oxindole privileged structure, while critically exploring these scaffolds' druglike properties. |
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Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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The application of isatin-based multicomponent-reactions in the quest for new bioactive and druglike moleculesBioactive compoundsIsatinMulticomponent reactionsOxindoleOxindole derivatives are known for their great interest in the field of Medicinal Chemistry, as they display vast biological activities. Recent efforts concerning the preparation of oxindole derivatives using isatin-based multicomponent reactions (MCRs) constitute a great advance in generating druglike libraries fast and with wide scaffold diversity. In this review, we address those recent developments, exploring the synthetic pathways and biological activities described for these compounds, namely antitumor, antibacterial, antifungal, antiparasitic, antiviral, antioxidant, anti-inflammatory and central nervous system (CNS) pathologies. To add new depth to this work, we used a well-established web-based free tool (SwissADME) to evaluate the most promising scaffolds in what concerns their druglike properties, namely by evaluating their compliance with some of the most valuable rules applied by medicinal chemists in both academia and industrial settings (Lipinski, Ghose, Veber, Egan, Muegge). The aim of this review is to endorse isatin-based MCRs as a valuable synthetic approach to attain new hit compounds bearing the oxindole privileged structure, while critically exploring these scaffolds' druglike properties.Elsevier Masson2021-02-05info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/articlehttp://hdl.handle.net/10316/93144http://hdl.handle.net/10316/93144https://doi.org/10.1016/j.ejmech.2020.113102eng02235234https://www.sciencedirect.com/science/article/pii/S0223523420310746Brandão, PedroMarques, CarolinaBurke, Anthony J.Pineiro, Martainfo:eu-repo/semantics/openAccessreponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos)instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informaçãoinstacron:RCAAP2022-05-25T06:06:58ZPortal AgregadorONG |
dc.title.none.fl_str_mv |
The application of isatin-based multicomponent-reactions in the quest for new bioactive and druglike molecules |
title |
The application of isatin-based multicomponent-reactions in the quest for new bioactive and druglike molecules |
spellingShingle |
The application of isatin-based multicomponent-reactions in the quest for new bioactive and druglike molecules Brandão, Pedro Bioactive compounds Isatin Multicomponent reactions Oxindole |
title_short |
The application of isatin-based multicomponent-reactions in the quest for new bioactive and druglike molecules |
title_full |
The application of isatin-based multicomponent-reactions in the quest for new bioactive and druglike molecules |
title_fullStr |
The application of isatin-based multicomponent-reactions in the quest for new bioactive and druglike molecules |
title_full_unstemmed |
The application of isatin-based multicomponent-reactions in the quest for new bioactive and druglike molecules |
title_sort |
The application of isatin-based multicomponent-reactions in the quest for new bioactive and druglike molecules |
author |
Brandão, Pedro |
author_facet |
Brandão, Pedro Marques, Carolina Burke, Anthony J. Pineiro, Marta |
author_role |
author |
author2 |
Marques, Carolina Burke, Anthony J. Pineiro, Marta |
author2_role |
author author author |
dc.contributor.author.fl_str_mv |
Brandão, Pedro Marques, Carolina Burke, Anthony J. Pineiro, Marta |
dc.subject.por.fl_str_mv |
Bioactive compounds Isatin Multicomponent reactions Oxindole |
topic |
Bioactive compounds Isatin Multicomponent reactions Oxindole |
description |
Oxindole derivatives are known for their great interest in the field of Medicinal Chemistry, as they display vast biological activities. Recent efforts concerning the preparation of oxindole derivatives using isatin-based multicomponent reactions (MCRs) constitute a great advance in generating druglike libraries fast and with wide scaffold diversity. In this review, we address those recent developments, exploring the synthetic pathways and biological activities described for these compounds, namely antitumor, antibacterial, antifungal, antiparasitic, antiviral, antioxidant, anti-inflammatory and central nervous system (CNS) pathologies. To add new depth to this work, we used a well-established web-based free tool (SwissADME) to evaluate the most promising scaffolds in what concerns their druglike properties, namely by evaluating their compliance with some of the most valuable rules applied by medicinal chemists in both academia and industrial settings (Lipinski, Ghose, Veber, Egan, Muegge). The aim of this review is to endorse isatin-based MCRs as a valuable synthetic approach to attain new hit compounds bearing the oxindole privileged structure, while critically exploring these scaffolds' druglike properties. |
publishDate |
2021 |
dc.date.none.fl_str_mv |
2021-02-05 |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.uri.fl_str_mv |
http://hdl.handle.net/10316/93144 http://hdl.handle.net/10316/93144 https://doi.org/10.1016/j.ejmech.2020.113102 |
url |
http://hdl.handle.net/10316/93144 https://doi.org/10.1016/j.ejmech.2020.113102 |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
02235234 https://www.sciencedirect.com/science/article/pii/S0223523420310746 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.publisher.none.fl_str_mv |
Elsevier Masson |
publisher.none.fl_str_mv |
Elsevier Masson |
dc.source.none.fl_str_mv |
reponame:Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) instname:Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação instacron:RCAAP |
instname_str |
Agência para a Sociedade do Conhecimento (UMIC) - FCT - Sociedade da Informação |
instacron_str |
RCAAP |
institution |
RCAAP |
reponame_str |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
collection |
Repositório Científico de Acesso Aberto de Portugal (Repositórios Cientìficos) |
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1777302755072802816 |