Synthesis and biological evaluation of 2-(arylethynyl)quinoline derivatives as mGluR5 antagonists for the treatment of neuropathic pain
- Synthesis and biological evaluation of 2-(arylethynyl)quinoline derivatives as mGluR5 antagonists for the treatment of neuropathic pain
- 손명희; 김지영; 임은정; 백두종; 최기항; 이재균; 배애님; 민선준; 조용서
- Metabotropic glutamate receptor; Antagonist; Quinoline; Sonogashira reaction; Neuropathic pain
- Issue Date
- Bioorganic & medicinal chemistry letters
- VOL 23, NO 5, 1472-1476
- We described here the synthesis and biological evaluation of mGluR5 antagonists containing a quinoline
ring structure. Using intracellular calcium mobilization assay (FDSS assay), we identified compound 5n,
showing high inhibitory activity against mGluR5. In addition, it was found that compound 5n has excellent
stability profile. Finally, this compound exhibited favorable analgesic effects in spinal nerve ligation
model of neuropathic pain, which is comparable to gabapentin.
- Appears in Collections:
- KIST Publication > Article
- Files in This Item:
There are no files associated with this item.
- RIS (EndNote)
- XLS (Excel)
Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.