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

Design, Synthesis, and Biological Evaluation of 6‐(2‐Amino‐substituted phenyl)‐4‐(substituted phenyl)‐1,2,4‐triazine‐3,5(2H,4H)‐dione Derivatives as Anticonvulsant Agents

“…A large number of synthetic heterocyclic compounds have been reported that display antiepileptic activities. Among them, 1,2,4‐triazine nucleus was selected because of a large number of biological activities of this heterocyclic nucleus such as anticonvulsant , anticancer , antimicrobial , anti‐HIV , anti‐inflammatory , analgesic , antidiabetic , antiasthmatic , antimalarial , and antianxiety . The newer anticonvulsant drug lamotrigine which bears 1,2,4‐triazine nucleus and acts through the continuation of voltage‐sensitive sodium ion (Na + ) channel inactivation appears to be valuable against all types of generalized seizures .…”

Synthesis of 2-(methylsulfonyl)-5-(4-(methylsulfonyl) phenyl)-4-phenyl-1H-[5-14C]imidazole, a selective COX-2 inhibitor, via asymmetrical benzoins

“…The overall host–guest interactions of selective inhibitors such as 4,5‐diarylimidazoles consist of hydrogen bond formation and van der waals forces . These stereoelectronic interactions can be affected by electron‐withdrawing and electron‐donating groups .…”

“…Unfortunately, these compounds are associated with adverse cardiovascular effects such as myocardial infarction, thrombosis and cardiac dysfunction. The most plausible reason for this effect is the suppression of COX‐2 dependent prostacyclin which mediates platelet activation and atherogenesis . Therefore, the search for a novel, structurally different and better pharmacodynamic profile of selective COX‐2 inhibitors devoid of the noted side effects is still an ongoing need for anti‐inflammatory therapy.…”

Design & synthesis of novel oxazolone & triazinone derivatives and their biological evaluation as COX-2 inhibitors

“…[13] Also, a series of 5-Aryl-6-(4-methylsulfonyl)-3-(metylthio)-1,2,4-triazine derivatives (5) which were evaluated for their COX-1/COX-2 inhibitory activity and showed strong inhibition of COX-2 over COX-1. [14] Moreover, 5, 6-diphenyl-1,2,4-triazin-3(2H)-one derivatives bearing 5-substituted 1,3,4-oxadiazole (6) were found to possess potent COX-2 inhibitory activity. [15] From the above findings and for design purpose it was useful to build on well-established structural features of selective COX-2 inhibitors based on oxazolone and triazinone moiety and mimicking the structure of well-known COX-2 inhibitors.…”