Synthesis, α-glucosidase inhibition, α-amylase inhibition, and molecular docking studies of 3,3-di(indolyl)indolin-2-ones

Santoso, Mardi and Ong, Li Lin and Aijijiyah, Nur Pasca and Wati, First Ambar and Azminah, Azminah and Annuur, Rose Malina and Fadlan, Arif and Judeh, Zaher M.A (2022) Synthesis, α-glucosidase inhibition, α-amylase inhibition, and molecular docking studies of 3,3-di(indolyl)indolin-2-ones. Heliyon, 8 (3). pp. 1-8.

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Official URL / DOI: https://doi.org/10.1016/j.heliyon.2022.e09045

Abstract

The synthesized 3,3-di(indolyl)indolin-2-ones 1a-p showed desired higher α-glucosidase inhibitory activities and lower α-amylase inhibitory activities than standard drug acarbose. Particularly, compound 1i showed favorable higher α-glucosidase % inhibition of 67 ± 13 and lower α-amylase % inhibition of 51 ± 4 in comparison to acarbose with % inhibition activities of 19 ± 5 and 90 ± 2, respectively. Docking studies of selected 3,3-di(indolyl)indolin-2-ones revealed key interactions with the active sites of both α-glucosidase and α-amylase, further supporting the observed % inhibitory activities. Furthermore, the binding energies are consistent with the % inhibition values. The results suggest that 3,3-di(indolyl)indolin-2-ones may be developed as suitable Alpha Glucosidase Inhibitors (AGIs) and the lower α-amylase activities should be advantageous to reduce the side effects exhibited by commercial AGIs.

Item Type: Article
Uncontrolled Keywords: 3,3-Di(indolyl)indolin-2-ones; Diabetes; α-glucosidase inhibition; α-amylase inhibition; Docking studie
Subjects: Q Science > QD Chemistry
Divisions: Faculty of Pharmacy > Department of Pharmacy
Depositing User: AZMINAH 204031
Date Deposited: 16 Mar 2022 08:21
Last Modified: 16 Mar 2022 08:21
URI: http://repository.ubaya.ac.id/id/eprint/41563

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