1370287-20-9

Basic information

• Product Name: N'-(3,5-difluoropyridin-4-yl)-3-phenylpropanehydrazide
• CAS NO: 1370287-20-9
• Molecular Weight: 277.274
• Mol File: 1370287-20-9.mol

Chemical Properties

• CAS DataBase Reference: N'-(3,5-difluoropyridin-4-yl)-3-phenylpropanehydrazide(CAS DataBase Reference)
• NIST Chemistry Reference: N'-(3,5-difluoropyridin-4-yl)-3-phenylpropanehydrazide(1370287-20-9)
• EPA Substance Registry System: N'-(3,5-difluoropyridin-4-yl)-3-phenylpropanehydrazide(1370287-20-9)

Safety Data

• Hazardous Substances Data: 1370287-20-9(Hazardous Substances Data)

Upstream product

• 851178-97-7 4-chloro-3,5-difluoro pyridine 

Relevant articles and documents

Novel Hydrazine Derivatives and Uses Thereof

The present invention provides various compounds and active ingredient P2X comprising novel hydrazine derivatives7 Composition for inhibiting receptor activity are disclosed. The invention relates to P2X7 Activity of receptors associated with various diseases, i.e. chronic inflammatory diseases, inflammatory pain, treatment of neuropathic pain, prevention or treatment of autoimmune diseases or degenerative disease can be useful. (by machine translation)

Structure-activity relationships and optimization of 3,5-dichloropyridine derivatives as novel P2X7 receptor antagonists

Screening of a library of chemical compounds showed that the dichloropyridine-based analogue 9 was a novel P2X7 receptor antagonist. To optimize its activity, we assessed the structure-activity relationships (SAR) of 9, focusing on the hydrazide linker, the dichloropyridine skeleton, and the hydrophobic acyl (R2) group. We found that the hydrazide linker and the 3,5-disubstituted chlorides in the pyridine skeleton were critical for P2X7 antagonistic activity and that the presence of hydrophobic polycycloalkyl groups at the R2 position optimized antagonistic activity. In the EtBr uptake assay in hP2X7-expressing HEK293 cells, the optimized antagonists, 51 and 52, had IC50 values of 4.9 and 13 nM, respectively. The antagonistic effects of 51 and 52 were paralleled by their ability to inhibit the release of the pro-inflammatory cytokine, IL-1β, by LPS/IFN-γ/BzATP stimulation of THP-1 cells (IC50 = 1.3 and 9.2 nM, respectively). In addition, 52 strongly inhibited iNOS/COX-2 expression and NO production in THP-1 cells, further indicating that this compound blocks inflammatory signaling and suggesting that the dichloropyridine analogues may be useful in developing P2X7 receptor targeted anti-inflammatory agents.