210568-69-7Relevant articles and documents
EOP, a newly synthesized ethyl pyruvate derivative, attenuates the production of inflammatory mediators via p38, ERK and NF-κB pathways in lipopolysaccharide-activated BV-2 microglial cells
Min, Soon,More, Sandeep Vasant,Park, Shin Young,Choi, Dong-Kug,Park, Ju-Young,Yoon, Sung-Hwa,Jeon, Sae-Bom,Park, Eun-Jung
, p. 19361 - 19375 (2014)
Microglia-induced neuroinflammation is an important pathological mechanism influencing various neurodegenerative disorders. Excess activation of microglia produces a myriad of proinflammatory mediators that decimate neurons. Hence, therapeutic strategies aimed to suppress the activation of microglia might lead to advancements in the treatment of neurodegenerative diseases. In this study, we synthesized a novel ethyl pyruvate derivative, named EOP (S-ethyl 2-oxopropanethioate) and studied its effects on lipopolysaccharide (LPS)-induced production of nitric oxide (NO) in rat primary microglia and mouse BV-2 microglia. EOP significantly decreased the production of NO, inducible nitric oxide synthase, cyclooxygenase and other proinflammatory cytokines, such as interleukin (IL)-6, IL-1β and tumor necrosis factor-α, in LPS-stimulated BV-2 microglia. The phosphorylation levels of extracellular regulated kinase, p38 mitogen-activated protein kinase, and nuclear translocation of NF-κB were also inhibited by EOP in LPS-activated BV-2 microglial cells. Overall, our observations indicate that EOP might be a promising therapeutic agent to diminish the development of neurodegenerative diseases associated with microglia activation.
Substances and Pharmaceutical Compositions for the Inhibition of Glyoxalases and Their Use As Anti-Fungal Agents
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Page/Page column 17-18, (2009/01/20)
The present invention pertains to substances of the formula (I) wherein X is O or S; and R1-R4 are defined in the claims as inhibitors of glyoxalase I and/or II, pharmaceutical compositions comprising one or more compounds according to formula (I) and the use of one or more compounds according to formula (I) for the treatment of diseases associated with increased glycolytic metabolism. In one embodiment, the disease is a fungal infection.
PTC sulfanylation of some carboxylic acids derivatives activated by α-sulfonyl or α-sulfinyl group, in solid-liquid system
Wladislaw, Blanka,Marzorati, Liliana,Donnici, Claudio L.,Biaggio, Francisco C.,Neves, Regina M. A.,Claro Jr., Nelson F.
, p. 197 - 208 (2007/10/03)
The sulfanylation of α-sulfonyl substituted lactone and thioesters and α-sulfinyl-substituted esters and thioesters, employing solid K2CO3, S-methyl methanethiosulfonate and TEBA, is reported. The results are compared with those in the homogeneous phase and in the non-catalytic two-phase system.
