Talks
Presentation Type
Oral Presentation
Discipline Track
Biomedical Science
Abstract Type
Research/Clinical
Abstract
Thiazolidinediones (TZDs) are a new class of antidiabetic drugs, having an insulin sensitizing effect in patients with type 2 diabetes. We report here the synthesis A series of thirteen 2,4-thiazolidinedione derivatives. The 2,4-thiazolidinedione ring's fifth position was used as a site for Knoevenagel condensation to generate the compounds listed in the title. The synthesised derivatives were characterised using a variety of physicochemical and spectral analyses, including IR, Mass, 1H-NMR, 13C-NMR, and elemental analysis. By using the carrageenan-induced rat paw edoema method, the alloxan-induced diabetes in wistar rats method, and the FRAP (ferric reducing antioxidant power) method, respectively, the derivatives were examined for their in vivo anti-diabetic, in vivo anti-inflammatory, and in vitro free radical scavenging activities. Some of the compounds showed promise as powerful anti-inflammatory, anti-free radical, and anti-diabetic medications. The most effective anti-diabetic compounds, NB7, NB12, and NB13, were docked using MOE software to study some potential structural insights into the potential binding patterns with the target PPAR active sites (PDB ID: 2PRG). The dichloro derivative chemical NB-7 has demonstrated strong anti-inflammatory and antioxidant potential in the current investigation in addition to having the highest anti-diabetic efficacy.
Recommended Citation
Chawla, Pooja A., "Synthesis, biological evaluation and molecular docking studies of novel 3,5- disubstituted 2,4-thiazolidinediones derivatives" (2023). Research Symposium. 24.
https://scholarworks.utrgv.edu/somrs/2022/talks/24
Included in
Synthesis, biological evaluation and molecular docking studies of novel 3,5- disubstituted 2,4-thiazolidinediones derivatives
Thiazolidinediones (TZDs) are a new class of antidiabetic drugs, having an insulin sensitizing effect in patients with type 2 diabetes. We report here the synthesis A series of thirteen 2,4-thiazolidinedione derivatives. The 2,4-thiazolidinedione ring's fifth position was used as a site for Knoevenagel condensation to generate the compounds listed in the title. The synthesised derivatives were characterised using a variety of physicochemical and spectral analyses, including IR, Mass, 1H-NMR, 13C-NMR, and elemental analysis. By using the carrageenan-induced rat paw edoema method, the alloxan-induced diabetes in wistar rats method, and the FRAP (ferric reducing antioxidant power) method, respectively, the derivatives were examined for their in vivo anti-diabetic, in vivo anti-inflammatory, and in vitro free radical scavenging activities. Some of the compounds showed promise as powerful anti-inflammatory, anti-free radical, and anti-diabetic medications. The most effective anti-diabetic compounds, NB7, NB12, and NB13, were docked using MOE software to study some potential structural insights into the potential binding patterns with the target PPAR active sites (PDB ID: 2PRG). The dichloro derivative chemical NB-7 has demonstrated strong anti-inflammatory and antioxidant potential in the current investigation in addition to having the highest anti-diabetic efficacy.