66742-57-2Relevant articles and documents
A Two Hour Synthesis of the Anti-Parkinson Drug Safinamide Methanesulfonate
Higa, Vanessa M.,Omori, Alvaro T.
supporting information, p. 1433 - 1436 (2021/07/20)
The critical moment of the COVID-19 outbreak requires a real-time supply of therapeutic agents. Thus, time economy in the synthesis of biologically active compounds has become increasingly decisive. In this work, we developed a two hour synthesis of the a
Morpholine amide derivative and application thereof
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Paragraph 0236; 0238-0241, (2020/12/14)
The invention discloses a morpholine amide derivative and application thereof, and particularly relates to a novel morpholine amide derivative and a pharmaceutical composition containing the compound.The invention also relates to a method for preparing th
Potential anti-neuroinflammatory NF-кB inhibitors based on 3,4-dihydronaphthalen-1(2H)-one derivatives
Sun, Yue,Zhou, Yan-Qiu,Liu, Yin-Kai,Zhang, Hong-Qin,Hou, Gui-Ge,Meng, Qing-Guo,Hou, Yun
, p. 1631 - 1640 (2020/08/19)
Nuclear factor kappa B (NF-кB) inhibition represents a new therapeutic strategy for the treatment of neuroinflammatory diseases. In this study, a series of 3,4-dihydronaphthalen-1(2H)-one (DHN; 6a-n, 7a-c) derivatives were synthesised and characterised by NMR and HRMS. We assessed the toxicity and anti-neuroinflammatory properties of these compounds and found that 6m showed the greatest anti-neuroinflammatory properties, with relatively low toxicity. Specifically, 6m significantly reduced reactive oxygen species production, down-regulated the expression of NOD-like receptor pyrin domain-containing protein 3 (NLRP3), apoptosis-associated speck-like protein containing a CARD (ASC), and caspase-1 and prevented lipopolysaccharide-stimulated BV2 microglia cells polarisation towards an M1 phenotype. Furthermore, 6m significantly decreased IκBα and NF-кB p65 phosphorylation, thus inhibiting the NF-кB signalling pathway. This suggests that 6m may be explored as a functional anti-neuroinflammatory agent for the treatment of inflammatory diseases in the central nervous system, such as multiple sclerosis, traumatic brain injury, stroke and spinal cord injury.