1456808-56-2

Upstream product

• 98-59-9 p-toluenesulfonyl chloride 
• 1209261-56-2 5,7-dihydroxy-4-methyl-3-(4-methylpiperazin-1-yl)-2H-chromen-2-one 
• 1456808-53-9 5-(3-((tert-butoxycarbonyl)amino)propoxy)-4-methyl-3-(4-methylpiperazin-1-yl)-2-oxo-2H-chromen-7-yl 4-methylbenzenesulfonate 
• 1456807-88-7 C₂₂H₂₄N₂O₆S 
• 1456807-82-1 C₂₉H₃₀N₂O₈S₂ 

Relevant academic research and scientific papers

Preparation of coumarin derivative thereof for the application of the major diseases in the brain

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.

Coumarin derivatives protect against ischemic brain injury in rats

Neuroprotection strategies are of great importance in the treatment of ischemic brain injury. Screening of our in-stock coumarin derivatives identified compound 1 as exhibiting neuroprotective activity. Subsequently, a structural optimization was carried out, which led to the discovery of the potent compound 20. This compound signi ficantly attenuated the damage in a cell line derived from a pheochromocytoma of the rat adrenal medulla induced by oxygen-glucose deprivation in vitro. Furthermore, compound 20 exhibited clear neuroprotection in middle cerebral artery occlusion rats by reducing infarct size and brain-water content, improving neurological function, and suppressing neuronal loss and neuropathological changes in the cortex and hippocampus. Pharmacokinetic evaluation indicated that compound 20 could penetrate the blood-brain barrier of rats.