A new series of selective COX-2 inhibitors: 5,6-diarylthiazolo[3,2-b][1,2,4]triazoles
L-768-277 was found to be a potent and selective COX-2 inhibitor.
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Exploring biological efficacy of coumarin clubbed thiazolo[3,2–b][1,2,4]triazoles as efficient inhibitors of urease: A biochemical and in silico approach
2020, International Journal of Biological MacromoleculesCitation Excerpt :Fused heterocyclic systems incorporating sulfur and nitrogen heteroatoms have emerged as useful scaffolds in medicinal chemistry research due to their multifaceted and noticeable biological properties [26-35]. Among these structures, a particular attention has been focused on thiazolotriazoles which contain a combination of thiazole and triazole rings, due to their diverse utility as antimicrobial [36-38], antipyretic [39], analgesic, anti–inflammatory [33,39-41], anticancer [42] and vasodilatory agents [43]. Recently, thiazolo[3,2–b][1,2,4] triazole compounds have also been explored as pharmacophoric elements for their enzymatic potential against butyrylcholinesterase for the treatment of Alzheimer’s disease, and α–glucosidase and α–amylase for the effective management of type 2 diabetes [44].
Medicinal chemistry of vicinal diaryl scaffold: A mini review
2019, European Journal of Medicinal ChemistryCitation Excerpt :Among those, thiadiazole analog 23 (ED50 = 0.7 mg/kg) was found to be more potent and selective towards COX-2 with free of gastrointestinal toxicity [23]. On further diversification on central heterocyclic ring, fused bicyclic system named imidazothiazole 24 (IC50 = 0.016 μM) [24] and thiazolotriazole 25 (IC50 = 0.003 μM) [25] was introduced and both series of the compounds showed good inhibitory activity. However, the latter analog showed superior pharmacokinetic profile compared to imidazothiazole analogs.
Biological Spectrum of Vicinal Diaryl-Substituted Fused Heterocycles
2018, Vicinal Diaryl Substituted Heterocycles: A Gold Mine for the Discovery of Novel Therapeutic AgentsFirst regioselective iodocyclization reaction of 3-aryl-5-(prop-2-ynylthio)-1H-1,2,4-triazoles
2015, Tetrahedron Letters