Design, synthesis, and biological evaluation of substituted 2-alkylthio-1,5-diarylimidazoles as selective COX-2 inhibitors

Navidpour, Latifeh; Shadnia, Hooman; Shafaroodi, Hamed; Amini, Mohsen; Dehpour, Ahmad Reza; Shafiee, Abbas

doi:10.1016/j.bmc.2006.12.041

Cited by 80 publications

(38 citation statements)

References 21 publications

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“…Recent studies revealed that the substituted imidazole derivatives have attracted much attention due to their broad spectrum of pharmacological activities such as anti-inflammatory, analgesic [75,76]. Literature survey shows that imidazole-heterocyclic compounds could be new classes of anticonvulsant agents by the virtue of their potential anticonvulsant properties [77].…”

Section: The Imidazole Functional Groupmentioning

confidence: 99%

Current Research on Antiepileptic Compounds

2015

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Epilepsy affects about 1% of the world's population. Due to the fact all antiepileptic drugs (AEDs) have some undesirable side effects and about 30% of epileptic patients are not seizure-free with the existing AEDs, there is still an urgent need for the development of more effective and safer AEDs. Based on our research work on antiepileptic compounds and other references in recent years, this review covers the reported work on antiepileptic compounds which are classified according to their structures. This review summarized 244 significant anticonvulsant compounds which are classified by functional groups according to the animal model data, although there are some limitations in the data. This review highlights the properties of new compounds endowed with promising antiepileptic properties, which may be proven to be more effective and selective, and possibly free of unwanted side effects. The reviewed compounds represent an interesting possibility to overcome refractory seizures and to reduce the percentage of patients with a poor response to drug therapy.

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Section: The Imidazole Functional Groupmentioning

confidence: 99%

Current Research on Antiepileptic Compounds

2015

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“…In contrast with the traditional NSAIDs which belong to different categories of chemical structures, selective COX-2 inhibitors can be classified into three groups ( Figure 1): (1) diaryl ethers with methanesulfonamide at position-2 of one ring, Nemisulide and CGP-28237 can be considered as lead compounds in this class 8 ; (2) trans-stilbenoids, such as resveratrol, a natural product found in grapes and other food products 9 ; (3) heterocyclic systems (such as 1,2,4 triazole 10,11 , imidazole 12 , pyrazol 13 , quinoline 14 , indol 15 , pyrimidine 16 , 1,2,4-triazine 17,18 ) with adjacent diaryl containing sulfamoyl (SO 2 NH 2 ) or methylsulfonyl (SO 2 Me) substitution at position-4 of one ring which exist in celecoxib, SC-558 and etoricoxib.…”

Section: Introductionmentioning

confidence: 99%

Structure-based design, synthesis, molecular docking study and biological evaluation of 1,2,4-triazine derivatives acting as COX/15-LOX inhibitors with anti-oxidant activities

Khoshneviszadeh

Shahraki

Khoshneviszadeh

et al. 2016

Journal of Enzyme Inhibition and Medicinal Chemistry

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A set of 1,2,4-triazine derivatives were designed as cyclooxygenase-2 (COX-2) inhibitors. These compounds were synthesized and screened for inhibition of cyclooxygenases (COX-1 and COX-2) based on a cellular assay using human whole blood (HWB) and lipoxygenase (LOX-15) that are key enzymes in inFammation. The results showed that 3-(2-(benzo-bis(4-methoxyphenyl)-1,2,4-triazine (G11) was identified as the most potent COX-2 inhibitor (78%) relative to COX-1 (50%). Ferric reducing anti-oxidant power (FRAP) assay revealed that compound G10 possesses the highest anti-oxidant activity. The compound G3 with IC 50 value of 124 mM was the most potent compound in LOX inhibitory assay. Molecular docking was performed and a good agreement was observed between computational and experimental results.

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“…They have a wide range of biological activities. They are well known analgesics, anti-inflammatory, antiparasitic, antihelmintic, platelet aggregation inhibitors and antiepileptic agents [9][10][11][12][13][14].…”

Section: Introductionmentioning

confidence: 99%