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https://hdl.handle.net/10316/107506
Title: | Ugi Adducts of Isatin as Promising Antiproliferative Agents with Druglike Properties | Authors: | Brandão, Pedro Puerta, Adrián Padrón, José M. Kuznetsov, Maxim L. Burke, Anthony J. Pineiro, Marta |
Keywords: | isatin; multicomponent reactions; Ugi reaction; Alzheimer’s disease; oxindole-lactam hybrids | Issue Date: | 2021 | Publisher: | Wiley Online Library | Project: | PD/BD/128490/2017–CATSUS UIDP/00313/2020 UIDB/50006/2020 UIDB/00313/2020 |
Serial title, monograph or event: | Asian Journal of Organic Chemistry (AsianJOC) | Volume: | 10 | Issue: | 12 | Abstract: | 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 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 inhibition, 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/10316/107506 | ISSN: | 2193-5807 2193-5815 |
DOI: | 10.1002/ajoc.202100684 | Rights: | embargoedAccess |
Appears in Collections: | I&D CQC - Artigos em Revistas Internacionais |
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Ugi reaction synthesis of oxindole-lactam _Brandao2021AsianJournalOrganicChemistry.pdf | 1.08 MB | Adobe PDF | View/Open |
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