4-oxothiazolidine has been researched along with 1-3-4-thiadiazole* in 1 studies
1 other study(ies) available for 4-oxothiazolidine and 1-3-4-thiadiazole
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Synthesis, biological evaluation and docking study of 1,3,4-thiadiazole-thiazolidinone hybrids as anti-inflammatory agents with dual inhibition of COX-2 and 15-LOX.
Selective inhibition of both cyclooxygenase-2 (COX-2) and 15-lipooxygenase (15-LOX) may provide good strategy for alleviation of inflammatory disorders while minimizing side effects associated with current anti-inflammatory drugs. The present study describes the synthesis, full characterization and biological evaluation of a series of thiadiazole-thiazolidinone hybrids bearing 5-alk/arylidene as dual inhibitors of these enzymes. Our design was based on merging pharmacophores that exhibit portent anti-inflammatory activities in one molecular frame. 5-(4-hydroxyphenyl)-1,3,4-thiadiazol-2-amine (3) was efficiently synthesized, chloroacetylated and cyclized to give the key 4-thiazolidinone (5). Knovenagel condensation of 5 with different aldehydes afforded the final compounds 6a-m, 7, 8 and 9. These compounds were subjected to in vitro COX-1/COX-2, 15-LOX inhibition assays. Compounds (6a, 6f, 6i, 6l, 6m and 9) with promising potency (IC Topics: Animals; Anti-Inflammatory Agents; Arachidonate 15-Lipoxygenase; Cyclooxygenase 2; Cyclooxygenase 2 Inhibitors; Edema; Humans; Lipoxygenase Inhibitors; Male; Molecular Docking Simulation; Rats; Thiadiazoles; Thiazolidines | 2018 |