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

Son, Myung-Hee; Kim, Ji Young; Lim, Eun Jeong; Baek, Du-Jong; Choi, Kihang; Lee, Jae Kyun; Pae, Ae Nim; Min, Sun-Joon; Cho, Yong Seo

doi:10.1016/j.bmcl.2012.12.056

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

Son, Myung-Hee;
Kim, Ji Young;
Lim, Eun Jeong;
Baek, Du-Jong;
Choi, Kihang;
외 4명

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초록

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. (c) 2012 Elsevier Ltd. All rights reserved.

키워드

Metabotropic glutamate receptor; Antagonist; Quinoline; Sonogashira reaction; Neuropathic pain; METABOTROPIC GLUTAMATE RECEPTORS; RAT MODEL; 2-METHYL-6-(PHENYLETHYNYL)-PYRIDINE MPEP; ALLOSTERIC MODULATORS; POTENT; ALLODYNIA; COGNITION; DISEASE; ANXIETY

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

저자: Son, Myung-Hee; Kim, Ji Young; Lim, Eun Jeong; Baek, Du-Jong; Choi, Kihang; Lee, Jae Kyun; Pae, Ae Nim; Min, Sun-Joon; Cho, Yong Seo

DOI: 10.1016/j.bmcl.2012.12.056

발행일: 2013-03-01

유형: Article

저널명: Bioorganic & Medicinal Chemistry Letters

권: 23

호: 5

페이지: 1472 ~ 1476

언어: ENG

출판사: PERGAMON-ELSEVIER SCIENCE LTD

발행국가: 영국

분량: 5 페이지

ISSN: E 1464-3405
P 0960-894X