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Attention has been focused on isatin-based oxindole scaffolds, for which promising results concerning butyrylcholinesterase BuChE inhibitory activity have previously been obtained. Considering some published reports and detailed analysis of the pharmacophores of commercially available drugs for AD powerful cholinesterase ChE inhibitors , we performed a strategic structural modification of the isatin core and generated a new family of isatin-based oxindole hybrids 27 new compounds possessing crucial key functional units in their framework. The syntheses were accomplished using multiple approaches, including simple N -alkylation reactions, copper-catalyzed amination reactions, and click chemistry. The resulting library was evaluated on ChE and MAO enzymes, both of which are involved in the pathophysiology of neurodegeneration. IC 50 values of 1. Received: 30 November Accepted after revision: 04 January Article published online: 16 February Year Archive Related E-Products. Download PDF. Synthesis ; 54 19 : DOI: Carolina S. Luisa Leitzbach. Holger Stark. Anthony J. Supporting Information. Google Scholar. Crossref PubMed. Article in Thieme Connect.
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