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 …

…, A Zarghi, F Montazer-Sadegh, A Shafiee…

Index: Irannejad, Hamid; Kebriaieezadeh, Abbas; Zarghi, Afshin; Montazer-Sadegh, Farhad; Shafiee, Abbas; Assadieskandar, Amir; Amini, Mohsen Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 2 p. 865 - 873

Full Text: HTML

Citation Number: 14

Abstract

Abstract 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 inhibition of COX-2 with IC 50 values in the range of 0.1–0.2 μM and in most cases had stronger anti- inflammatory and analgesic effects than indomethacin at doses 3 and 6 mg/kg. Among ...