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Construction of Spirooxindole Analogues Engrafted with Indole and Pyrazole Scaffolds as Acetylcholinesterase Inhibitors.

ABSTRACT: Twenty-five new hits of spirooxindole analogs 8a-y engrafted with indole and pyrazole scaffolds were designed and constructed via a [3+2]cycloaddition (32CA) reaction starting from three components: new chalcone-based indole and pyrazole scaffolds 5a-d, substituted isatins 6a-c, and secondary amines 7a-d. The potency of the compounds were assessed in modulating cholinesterase (AChE) activity using Ellman's method. Compounds 8i and 8y showed the strongest acetylcholine esterase inhibition (AChEI) with IC₅₀ values of 24.1 and 27.8 μM, respectively. Molecular docking was used to study their interaction with the active site of hAChE.

SUBMITTER: Islam MS

PROVIDER: S-EPMC8637602 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature

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Construction of Spirooxindole Analogues Engrafted with Indole and Pyrazole Scaffolds as Acetylcholinesterase Inhibitors.

Islam Mohammad Shahidul MS Al-Majid Abdullah Mohammed AM Azam Mohammad M Verma Ved Prakash VP Barakat Assem A Haukka Matti M Elgazar Abdullah A AA Mira Amira A Badria Farid A FA

ACS omega 20211112 47

Twenty-five new hits of spirooxindole analogs 8a-y engrafted with indole and pyrazole scaffolds were designed and constructed via a [3+2]cycloaddition (32CA) reaction starting from three components: new chalcone-based indole and pyrazole scaffolds 5a-d, substituted isatins 6a-c, and secondary amines 7a-d. The potency of the compounds were assessed in modulating cholinesterase (AChE) activity using Ellman's method. Compounds 8i and 8y showed the st ...[more]

PMID: 34869980

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