Biscoumarin analogs: Synthesis, α-glucosidase inhibitory potential and molecular docking study

• Published in: Malaysian Journal of Chemistry
• Main Author: Ahmat N.; Nik Abdullah Zawawi N.K.; Taha M.; Wadood A.; Rahim F.; Ullah H.
• Format: Article
• Language: English
• Published: Malaysian Institute of Chemistry 2020
• Online Access: https://www.scopus.com/inward/record.uri?eid=2-s2.0-85094925661&partnerID=40&md5=477a2fb23ddffc7683c81e172662e934

Eighteen biscoumarin analogs (1-18) were synthesized in moderately good yields and characterized by various spectroscopic methods. The biscoumarin analogs were further evaluated for α-glucosidase inhibitory potential. Amongst this series of 18 analogs, 15 analogs showed outstanding α-glucosidase inhibititory activity with IC50 values ranging from 14.39 ± 0.52 to 230.22 ± 0.83 μM when compared with the standard acarbose of IC50 value of 774.5 ± 1.94 μM, in which analog 4 was observed as the most active analog. Molecular docking study was carried out to understand the binding interaction of the compounds with the active site of α-glucosidase. Analog 4 was found to possess the most interaction with various proteins. This is in line with the findings in the α-glucosidase assay. © 2020 Malaysian Institute of Chemistry. All rights reserved.