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
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ACS OmegaAuthors
Date
2021Discipline
Epäorgaaninen ja analyyttinen kemiaEpäorgaaninen kemiaInorganic and Analytical ChemistryInorganic ChemistryCopyright
© 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.
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American Chemical Society (ACS)ISSN Search the Publication Forum
2470-1343Keywords
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https://converis.jyu.fi/converis/portal/detail/Publication/101880691
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The 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).License
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