title: Design, synthesis, and anti-inflammatory evaluation of novel diphenylthiazole-thiazolidinone hybrids.
abstract: A series of diphenylthiazole-thiazolidinone hybrids was synthesized and evaluated in vitro and in vivo as anti-inflammatory/analgesic agents. The inhibition of cyclooxygenase (COX) enzymes was suggested as a molecular mechanism for the hybrids to exert their anti-inflammatory action. Of these compounds, 13b, 14, and 15b showed the most potent COX inhibitory activity with IC50 values between 2.03 and 12.27 µM, but with different selectivity profiles. All compounds were further evaluated in vivo for their anti-inflammatory/analgesic activities using three animal models. Interestingly, the results of the COX assay were in agreement with those of in vivo assays where the most potent COX inhibitors, 13b, 14, and 15b, exhibited the highest anti-inflammatory/analgesic activities compared to diclofenac. On the contrary, compounds 11 and 12 were the least potent ligands in vitro and in vivo as well.
authors.affiliation: Department of Medicinal Chemistry, Faculty of Pharmacy, Beni-Suef University, Beni-Suef, Egypt.|Department of Pharmaceutical Chemistry, Taif University, Taif, Saudi Arabia.
authors.forename: Ahmed H
authors.initials: AH
authors.lastname: Abdelazeem
authors.affiliation: Department of Biochemistry, Faculty of Pharmacy, Al-Azhar University, Cairo, Egypt.|Department of Pharmacology, Division of Biochemistry and GTMR Unit, Taif University, Taif, Saudi Arabia.
authors.forename: Samir A
authors.initials: SA
authors.lastname: Salama
authors.affiliation: Department of Clinical Pharmacy, College of Pharmacy, Taif University, Taif, Saudi Arabia.
authors.forename: Ibrahim A
authors.initials: IA
authors.lastname: Maghrabi
mesh_terms: D000818:Animals; D051545:Cyclooxygenase 1 / Q000378:metabolism; D051546:Cyclooxygenase 2 / Q000378:metabolism; D016861:Cyclooxygenase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015195:Drug Design; D004487:Edema / Q000188:drug therapy; D006930:Hyperalgesia / Q000188:drug therapy; D051379:Mice; D062105:Molecular Docking Simulation; D011485:Protein Binding; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
chemical_list: D016861:Cyclooxygenase Inhibitors; D013844:Thiazoles; D051545:Cyclooxygenase 1; D051546:Cyclooxygenase 2
keywords: Anti-inflammatory/analgesic; COX; Diphenylthiazole-thiazolidinone hybrids; NSAIDs