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https://hdl.handle.net/10316/107441
Título: | Ugi Reaction Synthesis of Oxindole-Lactam Hybrids as Selective Butyrylcholinesterase Inhibitors | Autor: | Brandão, Pedro López, Óscar Leitzbach, Luisa Stark, Holger Fernández-Bolaños, José G. Burke, Anthony J. Pineiro, Marta |
Data: | 11-Nov-2021 | Editora: | ACS American Chemical Society | Projeto: | info:eu-repo/grantAgreement/FCT/POR_CENTRO/PD/BD/128490/2017/PT/Sustainable Asymmetric Catalytic Synthesis of Novel Oxindole Hybrids with Potential Biological Activity info:eu-repo/grantAgreement/FCT/UIDP/00313/2020 UIDB/50006/2020 UIDB/00313/2020 |
Título da revista, periódico, livro ou evento: | ACS Medicinal Chemistry Letters | Volume: | 12 | Número: | 11 | Resumo: | Molecular hybridization is a valuable approach in drug discovery. Combining it with multicomponent reactions is highly desirable, since structurally diverse libraries can be attained efficiently in an eco-friendly manner. In this work, isatin is used as the key building block for the Ugi 4-center 3-component reaction synthesis of oxindole-lactam hybrids, under catalyst-free conditions. The resulting oxindole-β-lactam and oxindole-γ-lactam hybrids were evaluated for their potential to inhibit relevant central nervous system targets, namely cholinesterases and monoamine oxidases. Druglikeness evaluation was also performed, and compounds 4eca and 5dab exhibited great potential as selective butyrylcholinesterase inhibitors, at the low micromolar range, with an interesting predictive pharmacokinetic profile. Our findings herein reported suggest oxindole-lactam hybrids as new potential agents for the treatment of Alzheimer's disease. | URI: | https://hdl.handle.net/10316/107441 | ISSN: | 1948-5875 | DOI: | 10.1021/acsmedchemlett.1c00344 | Direitos: | embargoedAccess |
Aparece nas coleções: | I&D CQC - Artigos em Revistas Internacionais |
Ficheiros deste registo:
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Brandao2021ACSMedChemLett.pdf | 2.89 MB | Adobe PDF | Ver/Abrir |
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