58848-77-4Relevant academic research and scientific papers
A new and facile synthesis of N-benzyl-N′-acylureas via reaction of dibenzoylhydrazine carboxamide and benzylamines
Valipour, Mehdi,Chippindale, Ann M.,Kouzeli, Aynaz,Irannejad, Hamid
, p. 3004 - 3012 (2021/08/12)
Herein, we report a new method of synthesis of N-acylureas (E1–5) via reaction of dibenzoylhydrazine carboxamide (N,2-bis(4-methoxybenzoyl)hydrazine-1-carboxamide) (C) and various benzylamines. Preparation of dibenzoylhydrazine carboxamide (C) was perform
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, Mehdi,Shahraki, Omolbanin,Khoshneviszadeh, Mahsima,Foroumadi, Alireza,Firuzi, Omidreza,Edraki, Najmeh,Nadri, Hamid,Moradi, Alireza,Shafiee, Abbas,Miri, Ramin
, p. 1602 - 1611 (2016/10/09)
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 in?ammation. The results showed that 3-(2-(benzo[d][1,3]dioxol-5-ylmethylene)hydrazinyl)-5,6-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 IC50 value of 124 μM was the most potent compound in LOX inhibitory assay. Molecular docking was performed and a good agreement was observed between computational and experimental results.
Microwave-assisted synthesis and anticonvulsant activity of 5,6-bisaryl-1,2,4-triazine-3-thiolderivatives
Irannejad, Hamid,Naderi, Nima,Emami, Saeed,Ghadikolaei, Roja Qobadi,Foroumadi, Alireza,Zafari, Tina,Mazar-Atabaki, Ali,Dadashpour, Sakineh
, p. 2503 - 2514 (2014/05/06)
A series of 5,6-bisaryl-1,2,4-triazine-3-thiol derivatives were synthesized through microwave-promoted chemistry by condensation of the aromatic 1,2-diketones and thiosemicarbazide in a mixed green solvent. Subsequently, S-alkylation of 1,2,4-triazine-3-t
In vitro antitumor activity evaluation of some 1,2,4-triazine derivatives bearing piperazine amide moiety against breast cancer cells
Yurtta, Leyla,Demirayak, eref,Ilgin, Sinem,Atli, ?zlem
, p. 6313 - 6323 (2015/01/09)
A series of 1,2,4-triazine derivatives bearing piperazine amide moiety has been synthesized and investigated for their potential anticancer activities. 1-[4-(5,6-Bis(4-subtituted phenyl)-1,2,4-triazin-3-yl)piperazin-1-yl]-2-[4-(3-substituted phenyl)pipera
Design, synthesis and biological evaluation of novel anti-cytokine 1,2,4-triazine derivatives
Khoshneviszadeh, Mehdi,Ghahremani, Mohammad H.,Foroumadi, Alireza,Miri, Ramin,Firuzi, Omidreza,Madadkar-Sobhani, Armin,Edraki, Najmeh,Parsa, Maliheh,Shafiee, Abbas
, p. 6708 - 6717 (2013/10/22)
A series of 16 novel 1,2,4-triazine derivatives bearing hydrazone moiety (7a-7p) have been designed, synthesized and evaluated for their activity to inhibit IL-1β and TNF-α production. All compounds are reported for the first time. The chemical structures of all compounds were confirmed by spectroscopic methods and elemental analyzes. Most of the synthesized compounds were proved to have potent anti-cytokine activity and low toxicity on PBMC and MCF-7 cell lines. Compounds 7f, 7k, 7l and 7j presented simultaneously good levels of inhibition of both cytokines. Moreover, compound 7l exhibited good anti-inflammatory effect in carrageenan-induced rat paw edema. The results of Western blotting demonstrated that the anti-cytokine potential of compound 7l is mainly mediated through the inhibition of p38 MAPK signaling pathway. Molecular docking was performed to position compound 7l into p38α binding site in order to explore the potential target. The information of this work might be helpful for the design and synthesis of novel scaffold toward the development of new therapeutic agent to fight against inflammatory diseases.
Attenuation of NF-κB and activation of Nrf2 signaling by 1,2,4-triazine derivatives, protects neuron-like PC12 cells against apoptosis
Tusi, Solaleh Khoramian,Ansari, Niloufar,Amini, Mohsen,Amirabad, Azim Dehghani,Shafiee, Abbas,Khodagholi, Fariba
experimental part, p. 738 - 751 (2011/02/25)
Oxidative stress has been implicated in the etiology of neurodegenerative diseases and aging. Indeed, accumulation of reactive oxygen species, such as hydrogen peroxide, generated by inflammatory cells, leads to oxidative stress, which may contribute to the neuronal degeneration observed in a wide variety of neurodegenerative disorders of the central nervous system, such as Alzheimer's disease. The present study indicates that H2O2-induced cell death can be inhibited in the presence of 1,2,4-triazine derivatives, as measured by MTT and caspase-3 activity. We further show that these compounds exert their protective effect by up-regulation of hemeoxygenase-1, glutamylcysteine synthetase, glutathione peroxidase and nuclear factor-erythroid 2 p45-related factor 2 (Nrf2), while they inhibit NF-κB and decrease lipid peroxidation. It shows that there is a potential cross talk between NF-κB and Nrf2, an important cytoprotective transcription factor in the presence of these compounds. Moreover, in order for drugs to be effective in the treatment of neurodegenerative diseases, they must be capable of penetrating the blood-brain barrier, whereas more than 98% of all potential central nervous system drugs don't cross. Using a reliable model based on the artificial neural network indicated that these compounds satisfy this requirement.
5,6-Diaryl-1,2,4-triazines as topical antithrombotic agents
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, (2008/06/13)
3-Substituted-5,6-diaryl-1,2,4-triazines active as antithrombotic agents when administered topically.
1,2,4-Triazine Chemistry. 10. Dihydro-1,2,4-triazines: Structural Studies of 5,6-Diaryldihydro-1,2,4-triazines through the Reactions with Dimethyl Acetylenedicarboxylate
Sasaki, Tadashi,Minamoto, Katsumaro,Harada, Katsuhiko
, p. 4587 - 4593 (2007/10/02)
Sodium borohydride reduction of 3-(methylthio)-5,6-diphenyl- (1a), 3-(methylthio)-5,6-ditolyl- (1c), 3-(methylthio)-5,6-dianisyl- (1e), and 3-(methylthio)-5,6-bis(p-chlorophenyl)-1,2,4-triazine (1g) afforded the corresponding 2,5-dihydro-1,2,4-triazines (
Pharmacologically active substituted 1,2,4-triazines
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, (2008/06/13)
Substituted 1,2,4-triazines, compositions thereof and methods of using same are described. The compounds of the invention exhibit a wide range of pharmacological activity including anti-inflammatory, analgesic, anti-pyretic, hypotensive and central nervous system effects.
5,6-Diaryl-1,2,4-triazines as topically-active anti-inflammatory agents
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, (2008/06/13)
A method of treating inflammation which utilizes topically-active 5,6-diaryl-1,2,4-triazines having the formula, STR1 wherein R is hydrogen or --(X)n R1, in which X is either O or S, n is an integer which is either 0 or 1, and R
