Polyhydroquinoline Derivatives for Diabetic Management: Synthesis, <i>in Vitro</i> and <i>in Silico</i> Approaches
Faiz Talab, Zainab Zainab, Aftab Alam, Mumtaz Ali, Najeeb Ur Rehman, Naeem Ullah, Sobia Ahsan Halim, Mohammad Shahidul Islam, Ajmal Khan, Abdul Latif, Muhammad Ayaz, Ahmed Al‐Ghafri, Ahmed Al‐Harrasi, Manzoor Ahmad
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.