Journal
ACS OMEGA
Volume 6, Issue 47, Pages 31539-31556Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsomega.1c03978
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- King Saud University, Riyadh, Saudi Arabia [RSP-2021/64]
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Twenty-five new hits of spirooxindole analogs engrafted with indole and pyrazole scaffolds were designed and constructed through a [3+2]-cycloaddition reaction. Compounds 8i and 8y showed the strongest acetylcholine esterase inhibition and were further studied with molecular docking for their interaction with the active site of hAChE.
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 chalconebased 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 mu M, respectively. Molecular docking was used to study their interaction with the active site of hAChE.
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