Pyrazoline scaffold: hit identification to lead synthesis and biological evaluation as antidiabetic agents.

Mining of novel scaffolds as potential DPP-IV inhibitors for future development of potential candidates as antidiabetic agents to address global issues. The identified hit from a previously reported study was taken as a lead for designing a library of analogues and screened initially based on parameters and docking score. A series of selected (2[4-(1-acetyl-5-phenyl-4,5-dihydro-1-pyrazol-3-yl)phenoxy]-1-phenylethanone derivatives were synthesized and evaluated through studies. Compounds , and were found to be as potent, with IC values of 0.10 μM, 0.12 μM and 0.35 μM, respectively. They also showed promising antihyperglycemic potential in studies (oral glucose tolerance tests) in Wistar rats. This work establishes pyrazoline analogues , and as promising starting points for the development of potential antidiabetic agents.