1209261-56-2Relevant academic research and scientific papers
Preparation of coumarin derivative thereof for the application of the major diseases in the brain
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Paragraph 0020; 0153; 0157, (2018/01/11)
The invention discloses novel coumarin compounds and pharmaceutically acceptable salts thereof, the preparation method of the compounds, pharmaceutical compositions containing the compounds, and application of the compounds to preparation of medicaments for prevention or treatment of cerebral diseases, especially prevention or treatment of diseases related to neuron damage and neuroinflammation, and prevention or treatment of Parkinson's disease, dementia, cerebral ischemia, depression and cerebral apoplexy.
Discovery and optimization of novel 3-piperazinylcoumarin antagonist Of chemokine-like factor 1 with oral antiasthma activity in mice
Li, Gang,Wang, Dongmei,Sun, Mingna,Li, Guangyan,Hu, Jinfeng,Zhang, Yun,Yuan, Yuhe,Ji, Haijie,Chen, Naihong,Liu, Gang
experimental part, p. 1741 - 1754 (2010/08/06)
Chemokine-like factor 1 (CKLF1) is a novel functional cytokine that acts through its receptor CC chemokine receptor 4 (CCR4). Activation of CCR4 by CKLF1 plays an important role in diseases such as asthma and multiple sclerosis. This article describes a cell-based screening assay using an FITC-labeled CCR4 agonist (CKLF1-C27), a CKLF1 peptide fragment. Screening of our in-stock smallmolecule library identified a 3-piperazinylcoumarin analogue 1 (IC 50 = 4.36 × 10-6 M) that led to the discovery of orally active compound, 41 (IC50 = 2.12 × 10-8 M) through systematic optimization. Compound 41 blocked the calcium mobilization and Chemotaxis induced, by CKLF1-C27 and reduced the asthmatic pathologic changes in lung tissue of human CKLF1-transfected mice. Further studies indicated that compound 41 ameliorated pathological changes via inhibition of the NF-κB signal pathway.
