Polyhydroquinoline Derivatives for Diabetic Management: Synthesis, in Vitro and in Silico Approaches
Faiz Talaba, Zainab Zainabb c, Aftab Alama, Mumtaz Alia, Najeeb Ur Rehmand e, Naeem Ullahd e, Sobia Ahsan Halimd e, Mohammad Shahidul Islamf, Ajmal Khand e, Abdul Latifa, Muhammad Ayaza, Ahmed Al‐Ghafrid e, Ahmed Al‐Harrasid e, Manzoor Ahmada
- aDepartment of Chemistry, University of Malakand, PO Box 18800, Dir Lower, Khyber Pakhtunkhwa, Pakistan
- bCollege of Chemistry &
- cMaterials Science, Hebei Normal University, Shijiazhuang, 050024, China
- dNatural &
- eMedical Sciences Research Center, University of Nizwa, Nizwa, 616, Oman
- fDepartment of Chemistry, College of Science, King Saud University, PO Box 2455, Riyadh, 11451, Saudi Arabia
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Abstract
Background: Medication used to treat Type 2 diabetes by decreasing the absorption of carbohydrates in the intestine consists of α-glucosidase inhibitors. Polyhydroquinoline derivatives have attracted interest as excellent antidiabetic agents. Methods: Polyhydroquinoline derivatives (1–17) were synthesized and tested for in vitro α-glucosidase inhibitory activity. Results: All the synthesized compounds exhibited excellent to good inhibitory activity, having IC50 values from 1.23 ± 0.03 to 73.85 ± 0.61 μM, compared with the standard drug, acarbose. The binding mechanism of these derivatives with α-glucosidase was deduced by docking studies and indicated that a slight variation in the orientation of compounds, affects their binding capability. Conclusion: In order to find new antidiabetic drugs, this study has discovered prospective lead candidates.
TL;DRIn order to find new antidiabetic drugs, this study has discovered prospective lead candidates based on the binding mechanism of Polyhydroquinoline derivatives with α-glucosidase and indicated that a slight variation in the orientation of compounds, affects their binding capability. (Semantic Scholar)