Please use this identifier to cite or link to this item: 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 
UIDB/00313/2020 
UIDP/00313/2020 
UIDB/50006/2020 
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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