163304-90-3Relevant 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
Dadashpour, Sakineh,Kucukkilinc, Tuba Tuylu,Tan, Oya Unsal,Ozadali, Keriman,Irannejad, Hamid,Emami, Saeed
, p. 179 - 187 (2015/03/14)
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
Irannejad, Hamid,Kebriaieezadeh, Abbas,Zarghi, Afshin,Montazer-Sadegh, Farhad,Shafiee, Abbas,Assadieskandar, Amir,Amini, Mohsen
, p. 865 - 873 (2014/02/14)
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
Investigations concerning the COX/5-LOX inhibiting and hydroxyl radical scavenging potencies of novel 4,5-diaryl isoselenazoles
Scholz, Michael,Ulbrich, Holger K.,Dannhardt, Gerd
, p. 1152 - 1159 (2008/09/20)
The aim of this study was to investigate 4,5-diaryl isoselenazoles as multiple target non-steroidal anti-inflammatory drugs (MTNSAIDs) which can intervene into the inflammatory processes via different mechanisms of action creating a new class of compounds
Syntheses of 4,5-diaryl-1,2,3-thiadiazoles
Karimi, Lila,Navidpour, Latifeh,Amini, Mohsen,Shafiee, Abbas
, p. 1593 - 1600 (2007/10/03)
Reaction of thionyl chloride with semicarbazones of 1-(4- methylsulfonylphenyl)-2-(4-substituted pheny)lethanone gave 4-(4- methylsulfonylphenyl)-5-(4-substituted) pheny-1,2,3-thiadiazoles 5. Compounds 5-phenyl-4-(substitutedphenyl)-1,2,3-thiadiazoles 14 were similarly prepared. Chlorosulfonation of the latter followed by ammonia gave the desired compounds 5-(4-aminosulfonylphenyl)-4-(substituted) phenyl-1,2,3-thiadiazoles 6. Copyright Taylor & Francis Inc.
Synthesis and biological evaluation of 2-phenylpyran-4-ones: A new class of orally active cyclooxygenase-2 inhibitors
Caturla, Francisco,Jiménez, Juan-Miguel,Godessart, Núria,Amat, Mercè,Cárdenas, Alvaro,Soca, Lídia,Beleta, Jordi,Ryder, Hamish,Crespo, María I.
, p. 3874 - 3886 (2007/10/03)
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.
