6533b86efe1ef96bd12cb4a8
RESEARCH PRODUCT
Construction of Spirooxindole Analogues Engrafted with Indole and Pyrazole Scaffolds as Acetylcholinesterase Inhibitors
Abdullah A. ElgazarMohammad Shahidul IslamMohammad Shahidul IslamFarid A. BadriaMatti HaukkaAmira MiraMohammad AzamVed Prakash VermaAssem BarakatAssem BarakatAbdullah Mohammed Al-majidsubject
Indole testChemistryStereochemistrybioaktiiviset yhdisteetGeneral Chemical EngineeringGeneral ChemistryPyrazoleindolespeptides and proteinsAcetylcholinesterasemolecular mechanicsArticleinhibitionchemistry.chemical_compoundChemistryscaffoldsQD1-999orgaaniset yhdisteetinhibiittoritdescription
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. peerReviewed
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2021-11-01 |