32362-88-2Relevant articles and documents
Analgesic and Anti-inflammatory Potential of Merged Pharmacophore Containing 1,2,4-triazoles and Substituted Benzyl Groups via Thio Linkage
Ahirwar,Ahirwar,Lanjhiyana,Jha,Dewangan,Badwaik
, p. 2130 - 2141 (2018)
A plethora of non-steroidal anti-inflammatory drugs are available in the market with adverse side effects like gastrointestinal irritation, bleeding, and ulceration. Currently, the focus of researcher on the development of better, synergistic molecules by the hybridization of two or more active biomolecule or ligands to develop newer derivative possessing good anti-inflammatory activity with minimum side effects. In line with this, the present study was designed to synthesize a series of merged pharmacophore contaning1,2,4-triazoles and substituted benzyl groups via thio linkage. Purity of the derivatives was confirmed by thin-layer chromatography, combustion analysis, and melting point. Structure of these derivatives was set up by determining infrared spectroscopy, nuclear magnetic resonance spectroscopy, and mass spectroscopy. All the synthesized derivatives were evaluated for their analgesic and anti-inflammatory activities in mice and rats, respectively. In animal studies, the derivative 3-(5-(4-nitrobenzylthio)-4H-1,2,4-triazol-3-yl) pyridine showed more potent analgesic activity, and the derivative 3-(5-(2,4-dimethylbenzylthio)-4H-1,2,4-triazol-3-yl) pyridine showed more potent anti-inflammatory activity as compared with other derivatives. The results of the present study indicate that reaction of pyridine linked 1,2,4-triazole-3-thiol with different substituted benzyl halides to produce merged pharmacophore contaning1,2,4-triazoles and substituted benzyl groups with potent analgesic and anti-inflammatory activities. Docking studies were performed by using Argus lab, and all the derivatives exhibited good docking scores between ?10 and ?12?kcal/mol and were better as compared with standard drugs aspirin and indomethacin against cyclooxygenase-2. Among all compounds, 3j has shown the maximum docking score and found in agreement to in pharmacological activities.
Novel synthesis of condensed heterocyclic systems containing 1,2,4-triazole ring
Wang,Shi,Shi
, p. 2841 - 2848 (2001)
3-Aryl-6,7-dihydro-s-triazolo[3,4-b][1,3]thiazines and 3-aryl-5,6-dihydro-thiazolo[2,3-c]-s-triazoles were synthesized by nucleophilic substitution of 3-aryl-5-mercapto-1,2,4-triazoles with 1,3-dibromopropane and 1,2-dichloroethane. And the bis-Mannich re
Heterocycles 39. Synthesis, characterization and evaluation of the anti-inflammatory activity of thiazolo[3,2-b][1,2,4]triazole derivatives bearing pyridin-3/4-yl moiety
Toma, Alexandra,Mogo?an, Cristina,Vlase, Laurian,Leonte, Denisa,Zaharia, Valentin
, p. 2602 - 2613 (2017/10/06)
Abstract: A series of pyridin-3/4-yl-thiazolo[3,2-b][1,2,4]triazole derivatives (5a–g, 6a–g) were synthesised by Hantzsch condensation of 5-pyridin-3/4-yl-1,2,4-triazole-3-thiol and diverse α-halocarbonyl compounds. Different reaction conditions (pH, temperature, solvent) were investigated for the efficient obtention of the target compounds. Under reflux and acidic conditions, the Hantzsch condensation was a one-step reaction. At room temperature and under basic conditions, it was possible to isolate the iminothioether intermediates 3/4a–g. These intermediates were cyclized in a subsequent step by treatment with concentrated sulphuric acid. The obtained compounds were evaluated for their anti-inflammatory activity. Three synthesised pyridyl-thiazolo[3,2-b][1,2,4]triazole derivatives (6c, 6d, 6f) were found to be good anti-inflammatory agents. Graphical Abstract: [InlineMediaObject not available: see fulltext.].
