Author/Authors :
Ahmat, Norizan Faculty of Applied Sciences - UiTM Shah Alam - 40450 Shah Alam - Selangor D.E. Malaysia - Atta-ur-Rahman Institute for Natural Product Discovery - Universiti Teknologi MARA (UiTM) - Puncak Alam Campus - 42300 Bandar Puncak Alam - Selangor D. E. Malaysia , Nik Abdullah Zawawi, Nik Khairunissa Faculty of Applied Sciences - UiTM Shah Alam - 40450 Shah Alam - Selangor D.E. Malaysia , Taha, Muhammad Atta-ur-Rahman Institute for Natural Product Discovery - Universiti Teknologi MARA (UiTM) - Puncak Alam Campus - 42300 Bandar Puncak Alam - Selangor D. E. Malaysia , Wadood, Abdul Department of Chemistry - Abdul Wali Khan University Mardan - Khyber Pakhtunkhwa, Pakistan , Rahim, Fazal Department of Chemistry - Hazara University Mansehra - 21300 Khyber Pakhtunkhwa, Pakistan , Ullah, Hayat Department of Chemistry - Hazara University Mansehra - 21300 Khyber Pakhtunkhwa, Pakistan
Abstract :
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.
Keywords :
Synthesis , biscoumarin , α-glucosidase inhibition , Molecular docking study , SAR
