Polyhydroquinoline derivatives for diabetic management: synthesis, in vitro and in silico approaches.
Faiz Talabnull ZainabAftab AlamMumtaz AliNajeeb Ur RehmanSaeed UllahSobia Ahsan HalimMohammad Shahidul IslamAjmal KhanAbdul LatifMuhammad AyazAhmed Al-GhafriAhmed Al-HarrasiManzoor AhmadPublished in: Future medicinal chemistry (2023)
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 IC 50 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.