Synthesis and biological evaluation of thiazolidine-2,4-dione-pyrazole conjugates as antidiabetic, anti-inflammatory and antioxidant agents.
A series of fourteen novel thiazolidine-2,4-dione derivatives clubbed with pyrazole moiety were synthesized via four step reaction procedure. Reactions were monitored by thin layer chromatography and were characterized by physicochemical and spectrophotometric (IR, Mass, 1HNMR and 13CNMR) analysis. The spectral data were in good agreement with their structures. The title compounds were docked against peroxisome proliferated activated receptors (PPAR-γ) and alpha-amylase and further evaluated for in vivo and in vitro antidiabetic, in vitro anti-inflammatory and antioxidant activities. Compound GB14 exhibited significant blood glucose lowering activity and was also found to be active inhibitor of alpha-amylase. Compound GB7 was found to be potent anti-inflammatory agent in terms of reducing inflammatory markers (TNF-α, IL-β, MDA) and also showed antioxidant activity to good extent. Therefore, these compounds may be considered as promising candidates for the development of new antidiabetic agents.
['Bansal|Garima|G|', 'Singh|Shamsher|S|', 'Monga|Vikramdeep|V|', 'Thanikachalam|Punniyakoti Veeraveedu|PV|', 'Chawla|Pooja|P|']
D000818:Animals D000894:Anti-Inflammatory Agents, Non-Steroidal D000975:Antioxidants D001786:Blood Glucose D004305:Dose-Response Relationship, Drug D007004:Hypoglycemic Agents D053583:Interleukin-1beta D008315:Malondialdehyde D051379:Mice D008810:Mice, Inbred C57BL D062105:Molecular Docking Simulation D015394:Molecular Structure D047495:PPAR gamma D011720:Pyrazoles D013329:Structure-Activity Relationship D045162:Thiazolidinediones D014409:Tumor Necrosis Factor-alpha D000516:alpha-Amylases
Antidiabetic Anti-inflammatory Antioxidant Thiazolidine-2,4-dione PPAR-γ Alpha amylase