Construction of Spirooxindole Analogues Engrafted with Indole and Pyrazole Scaffolds as Acetylcholinesterase Inhibitors
Islam, M. S., Al-Majid, A. M., Azam, M., Verma, V. P., Barakat, A., Haukka, M., Elgazar, A. A., Mira, A., & Badria, F. A. (2021). Construction of Spirooxindole Analogues Engrafted with Indole and Pyrazole Scaffolds as Acetylcholinesterase Inhibitors. ACS Omega, 6(47), 31539-31556. https://doi.org/10.1021/acsomega.1c03978
Published inACS Omega
DisciplineEpäorgaaninen ja analyyttinen kemiaEpäorgaaninen kemiaInorganic and Analytical ChemistryInorganic Chemistry
© XXXX The Authors. Published by American Chemical Society
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.
PublisherAmerican Chemical Society (ACS)
Publication in research information system
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Additional information about fundingThe authors would like to extend their sincere appreciation to the Deanship of Scientific Research at King Saud University for providing funding to this Research group NO (RGP-257).
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