Twenty-five new hits of spirooxindole analogs engrafted with indole and pyrazole scaffolds were designed and constructed a [3+2]cycloaddition (32CA) reaction starting from three components: new chalcone-based indole and pyrazole scaffolds , substituted isatins , and secondary amines . The potency of the compounds were assessed in modulating cholinesterase (AChE) activity using Ellman's method. Compounds and showed the strongest acetylcholine esterase inhibition (AChEI) with IC values of 24.1 and 27.8 μM, respectively. Molecular docking was used to study their interaction with the active site of hAChE.
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| http://dx.doi.org/10.1021/acsomega.1c03978 | DOI Listing |
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