X-ray crystal structure of rivoglitazone bound to PPARγ and PPAR subtype selectivity of TZDs

VCE‐004.3, a cannabidiol aminoquinone derivative, prevents bleomycin‐induced skin fibrosis and inflammation through PPARγ‐ and CB2 receptor‐dependent pathways

“…Docking analysis was performing using AutoDock4 (Morris et al, 2009) and Vina softwares (Trott and Olson, 2010) with the virtual screening tool PyRx (Wolf, 2009) and PyMOL (Baugh et al, 2011). The receptor model used was the Protein Data Bank (PDB) reference (RCSB PDB accession code), 3B0R (Hughes et al, 2014), and 5U5L (Rajapaksha et al, 2017). The search space for the docking was set according to previous findings about several binding sites for different ligands.…”

Design, Synthesis, Antihyperglycemic Studies, and Docking Simulations of Benzimidazole-Thiazolidinedione Hybrids

“…PPARc controls target genes involved in several biological processes, for example, the facilitated glucose transporter GLUT-4 [3]. e thiazolidine-2,4-dione ring in most of the antidiabetic glitazones, such as pioglitazone and rosiglitazone, is accompanied by an additional nitrogencontaining heterocycle, for example, pyridine [4][5][6]. iazolidine-2,4-diones could be considered synthetic acid bioisosteres of natural antidiabetic p-coumaric acid [7,8].…”

“…In this work, we chose the benzimidazole azaheterocycle to generate the antihyperglycemic hybrids because this scaffold is of great importance due to its appreciated pharmacological actions in medicinal chemistry and applications in organic synthesis, acting as a privileged structure [3,[9][10][11], which can selectively modulate diverse targets associated with the pathogenesis of diabetes. On the other hand, the election of benzylidenethiazolidine-2,4-dione as p-coumaric acid bioisostere (the major natural component widely found in grapes, red wine, tomatoes, spinach, garlic, and coffee) was taken into account because several acid bioisosteres have demonstrated antidiabetic effects [4][5][6][7][8].…”

Synthesis of Novel Thiazolidin‐4‐ones and Thiazinan‐4‐ones Analogous to Rosiglitazone

“…TZDs target the nuclear receptor peroxisome proliferator activated receptor gamma and include rosiglitazone, pioglitazone, and troglitazone drugs (Fig. ) .…”