404966-41-2

Upstream product

• 35675-44-6 4-methylphenylacetyl chloride 
• 622-47-9 4-tolylacetic acid 
• 100-68-5 methyl-phenyl-thioether 
• 708276-16-8 2-(4-methylphenyl)-1-(4-methylsulfanylphenyl)ethanone 

Downstream Products

• 1026042-79-4 3-chloro-3-(4-methanesulfonyl-phenyl)-2-p-tolyl-acrylonitrile 
• 1542256-73-4 6-(4-(methylsulfonyl)phenyl)-3-(methylthio)-5-(p-tolyl)-1,2,4-triazine 
• 1542256-63-2 C₁₆H₁₅NO₄S 
• 1542256-68-7 C₁₇H₁₅N₃O₂S₂ 
• 328553-88-4 5-(4-methanesulfonyl-phenyl)-4-p-tolyl-1H-pyrazol-3-ylamine 

Relevant academic research and scientific papers

Design, synthesis and in vitro study of 5,6-diaryl-1,2,4-triazine-3-ylthioacetate derivatives as COX-2 and β-amyloid aggregation inhibitors

In order to find novel cyclooxygenase (COX)-2 inhibitors for treating inflammatory-based diseases such as Alzheimer's disease (AD), an ethyl carboxylate side chain was added to 5-(4-chlorophenyl)-6-(4-(methylsulfonyl)phenyl)-3-(methylthio)-1,2,4-triazine

Synthesis, docking simulation, biological evaluations and 3D-QSAR study of 5-Aryl-6-(4-methylsulfonyl)-3-(metylthio)-1,2,4-triazine as selective cyclooxygenase-2 inhibitors

A series of 5-Aryl-6-(4-methylsulfonyl)-3-(metylthio)-1,2,4-triazine derivatives were synthesized and their COX-1/COX-2 inhibitory activity as well as in vivo anti-inflammatory and analgesic effects were evaluated. All of compounds showed strong inhibitio

Synthesis and biological evaluation of 2-phenylpyran-4-ones: A new class of orally active cyclooxygenase-2 inhibitors

A series of 2-phenylpyran-4-ones were prepared and evaluated for their ability to inhibit cyclooxygenase-2 (COX-2). Extensive structure-activity relationship work was carried out within this series, and a number of potent and selective COX-2 inhibitors were identified. Compounds having a p-methylsulfone group at the 2-phenyl ring showed the best COX-2 inhibitory activity. The introduction of a substituted phenoxy ring at position 3 enhanced both the in vitro and in vivo activity within the series. A selected group of 3-phenoxypyran-4-ones exhibited excellent activity in an experimental model of pyresis. The in vivo antiinflammatory activity of these compounds was confirmed with the evaluation of their antiarthritic and analgesic effectiveness. Moreover, their pharmacokinetic profile in rats is compatible with a once a day administration by oral route in humans. Within this novel series, compounds 21, 31, 34, and 35 have been selected for further preclinical and clinical evaluation.

Synthesis and SAR of a new series of COX-2-selective inhibitors: Pyrazolo[1,5-α]pyrimidines

The synthesis and pharmacological activity of a series of bicyclic pyrazolo[1,5-α]pyrimidines as potent and selective cyclooxygenase-2 (COX-2) inhibitors are described. The new compounds were evaluated both in vitro (COX-1 and COX-2 inhibition in human whole blood) and in vivo (carrageenan-induced paw edema and air-pouch model). Modification of the pyrimidine substituents showed that 6,7-disubstitution provided the best activity and led to the identification of 3-(4-fluorophenyl)-6,7-dimethyl-2-(4-methylsulfonylphenyl) pyrazolo[1,5-α]pyrimidine (10f) as one of the most potent and selective COX-2 inhibitor in this series.