79074-45-6Relevant articles and documents
Intramolecular Diels-Alder reaction of pyrazines with an alkenyl side chain
Chen, Bin,Yang, Chu-Yao,Ye, De-Yong
, p. 8205 - 8208 (1996)
Intramolecular Diels-Alder reaction of a series of pyrazines bearing a 5-membered-ω-alkene side chain in refluxing trifluoroacetic acid led to the formation of bridged tricyclic compounds. These cycloadducts underwent Retro Diels-Alder reaction in refluxing nitrobenzene to give original pyrazines.
Design, synthesis and anti-inflammatory evaluation of novel 5-benzylidene-3,4-dihalo-furan-2-one derivatives
Wang, Fang,Sun, Jun-Rong,Huang, Mei-Yan,Wang, Hui-Ying,Sun, Ping-Hua,Lin, Jing,Chen, Wei-Min
, p. 35 - 45 (2014)
Rosiglitazone has shown promising anti-inflammation effect. To develop preferable anti-inflammatory agents, twenty-two rosiglitazone analogs were synthesized and their anti-inflammatory activity was evaluated. Among these compounds, 6i and 6k displayed excellent inhibitory activities on the production of inflammatory mediators, including nitric oxide (NO), tumor necrosis factor-alpha (TNF-α) and interleukin-6 (IL-6). Furthermore, 6i and 6k showed suppression effects on the nuclear factor-kappa B (NF-κB) and mitogen-activated protein kinase (MAPK) pathways, and this suppression effects could be partially reversed by GW9662, which is a peroxisome proliferator-activated receptor γ (PPARγ) antagonist. Additionally, our docking results exhibited the well combination of 6i and 6k to PPARγ. So the anti-inflammation activity of 6i and 6k was due at least in part, to their interaction with PPARγ.
Novel Oxazolidinone Antibacterial Analogues with a Substituted Ligustrazine C-ring Unit
Chen, Yan,Ruan, Zhi-Xiong,Wang, Fang,Huangfu, De-Sheng,Sun, Ping-Hua,Lin, Jing,Chen, Wei-Min
, p. 682 - 690 (2015)
A series of novel oxazolidinone compounds with a substituted ligustrazine C-ring unit and different substituted groups at the C-5 side chain were designed and synthesized using linezolid as a lead and based on a scaffold hopping strategy. Their antibacterial and anti-inflammatory activities were evaluated. The results of in vitro antibacterial assays showed that all fourteen target compounds displayed potent activity against Gram-positive pathogens, particularly 8b, 13b, 14a, 14b, 15a, and 15b. Moreover, 14a and 14b exhibited significant inhibitory activities on the production of inflammatory mediators, including nitric oxide, interleukin-6, and tumor necrosis factor-alpha. Thus, these derivatives could serve as valuable candidates to develop anti-infective agents for the treatment of chronic wounds.
Application of pyrazine compound in preparation of drugs
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Paragraph 0072-0074, (2020/10/30)
The invention relates to an application of a pyrazine compound in preparation of drugs. The drugs can be used for treating neurodegenerative diseases including Alzheimer's disease, Parkinson's disease, Huntington's disease, frontotemporal dementia (FTD), vascular dementia, HIV-related dementia, multiple sclerosis, progressive lateral sclerosis, Friedreich's ataxia, neuropathic pain or glaucoma, inflammation, oxidative damage, and mitochondrial-related diseases.
Ligustrazine/azoonium diol salt derivative as well as preparation method and application thereof
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Paragraph 0022; 0025-0026, (2019/12/02)
The invention discloses a ligustrazine/azoonium diol salt derivative as well as a preparation method and application thereof. The derivative has a structure as shown in a formula (I) which is described in the specification, wherein R1 and R2 are the same or different; the R1 and R2 are the same or different and independently represent a hydrogen atom and a C1-C4 alkyl group, and the R1 and R2 forma 5- to 7-membered aliphatic heterocyclic ring or aromatic heterocyclic ring along with the nitrogen atom to which R1 and R2 are connected.; the aliphatic heterocycle or the aromatic heterocycle maybe optionally mono-substituted to penta-substituted by the same or different substituents, the substituents being a C1-C6 alkyl group, a C1-C6 alkoxy group, a hydroxyl group, or a halogen. The ligustrazine/azoonium diol salt derivative provided by the invention can inhibit proliferation of tumor cells to different extents. Besides, compared with common breast cancer cells, the ligustrazine/azoonium diol salt derivative provided by the invention has a stronger proliferation inhibition effect on drug-resistant breast cancer cells, and prompts that the ligustrazine/azoonium diol salt derivative has a good application prospect on drug-resistant tumors.