1473385-86-2

Upstream product

• 1308631-40-4 N-(4-chloro-2-fluorophenyl)-2-hydroxybenzamide 
• 79-22-1 methyl chloroformate 
• 69-72-7 salicylic acid 
• 1441-87-8 salicyloyl chloride 

Relevant academic research and scientific papers

Modified salicylanilide and 3-phenyl-2 H -benzo[ e ][1,3]oxazine-2,4(3 H)-dione derivatives as novel inhibitors of osteoclast differentiation and bone resorption

Inhibition of osteoclast formation is a potential strategy to prevent inflammatory bone resorption and to treat bone diseases. In the present work, the purpose was to discover modified salicylanilides and 3-phenyl-2H-benzo[e][1,3]oxazine-2,4(3H)-dione derivatives as potential antiosteoclastogenic agents. Their inhibitory effects on RANKL-induced osteoclastogenesis from RAW264.7 cells were evaluated by TRAP stain assay. The most potent compounds, 1d and 5d, suppressed RANKL-induced osteoclast formation and TRAP activity dose-dependently. The cytotoxicity assay on RAW264.7 cells suggested that the inhibition of osteoclastic bone resorption by these compounds did not result from their cytotoxicity. Moreover, both compounds downregulated RANKL-induced NF-κB and NFATc1 in the nucleus, suppressed the expression of osteoclastogenesis-related marker genes during osteoclastogenesis, and prevented osteoclastic bone resorption but did not impair osteoblast differentiation in MC3T3-E1. Therefore, these modified salicylanilides and 3-phenyl-2H-benzo[e][1,3]oxazine-2,4(3H)-diones could be potential lead compounds for the development of a new class of antiresorptive agents.

PHARMACEUTICAL COMPOSITION OF SALICYLANILIDE-DERIVED SMALL MOLECULES AND PREPARATION AND APPLICATION THEREOF

The present invention provides a pharmaceutical composition of salicylanilide-derived small molecules include: (a) a compound which structure is selected from formula I or formula II: (b) a pharmaceutically acceptable salt and excipient. The present invention also provides the synthesis method of the pharmaceutical composition and the application thereof.