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Title: The application of isatin-based multicomponent-reactions in the quest for new bioactive and druglike molecules
Authors: Brandão, Pedro 
Marques, Carolina
Burke, Anthony J. 
Pineiro, Marta 
Keywords: Bioactive compounds; Isatin; Multicomponent reactions; Oxindole
Issue Date: 5-Feb-2021
Publisher: Elsevier Masson
Project: PD/BD/128490/2017 
Serial title, monograph or event: European Journal of Medicinal Chemistry
Volume: 211
Abstract: 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.
ISSN: 02235234
DOI: 10.1016/j.ejmech.2020.113102
Rights: embargoedAccess
Appears in Collections:I&D CQC - Artigos em Revistas Internacionais

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