SYNTHESIS, MOLECULAR DOCKING AND ANTIDIABETIC ACTIVITY OF SOME SULPHONAMIDE BEARING QUINAZOLINONE MOIETIES
Shweta S. Gaikwad*, Shailaja B. Jadhav and Deepti D. Banadawane
ABSTRACT
Type 2 diabetes (T2D) is a lifestyle disease affecting millions of people worldwide. Herein, the design and synthesis of 17 novel quinazolinone incorporating sulphonamide scaffold are described. Designed compound were docked using AutoDock (4.2.6) tool software with DPP-IV inhibitor protein (PDB: 3OPM). Synthesized compounds (4a-q) were evaluated for antidiabetic activity in streptozotocin-nicotinamide induced diabetic rats. Most of these synthesized compounds showed significant reduction in blood glucose level. Amongst all the compounds designed in this study, we identified compound 4q as a potent, selective and orally active antidiabetic agent, which exhibited in vivo efficacy in diabetic rat model.
Keywords: Antidiabetic agents, Quinazolinone, Sulphonamide, Type 2 Diabetes.
[Full Text Article]
[Download Certificate]