Synthesis and biological evaluation of 2-(arylethynyl)quinoline derivatives as mGluR5 antagonists for the treatment of neuropathic pain

Title
Synthesis and biological evaluation of 2-(arylethynyl)quinoline derivatives as mGluR5 antagonists for the treatment of neuropathic pain
Authors
손명희김지영임은정백두종최기항이재균배애님민선준조용서
Keywords
Metabotropic glutamate receptor; Antagonist; Quinoline; Sonogashira reaction; Neuropathic pain
Issue Date
2013-03
Publisher
Bioorganic & medicinal chemistry letters
Citation
VOL 23, NO 5, 1472-1476
Abstract
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.
URI
http://pubs.kist.re.kr/handle/201004/45198
ISSN
0960894X
Appears in Collections:
KIST Publication > Article
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