Discovery and biological evaluation of tetrahydrothieno[2,?3-?c]?pyridine derivatives as selective metabotropic glutamate receptor 1 antagonists for the potential treatment of neuropathic pain

Title
Discovery and biological evaluation of tetrahydrothieno[2,?3-?c]?pyridine derivatives as selective metabotropic glutamate receptor 1 antagonists for the potential treatment of neuropathic pain
Authors
남민아김태훈곽진숙서선희고민경임은정민선준조용서금교창백두종이지연배애님
Keywords
mGluR1; Metabotropic glutamate receptor; Neuropathic pain; Thiophene derivatives
Issue Date
2015-06
Publisher
European journal of medicinal chemistry
Citation
VOL 97, 245-258
Abstract
Metabotropic glutamate receptor 1 (mGluR1) has been a prime target for drug discovery due to its heavy involvement in various brain disorders. Recent studies suggested that mGluR1 is associated with chronic pain and can serve as a promising target for the treatment of neuropathic pain. In an effort to develop a novel mGluR1 antagonist, we designed and synthesized a library of compounds with tetrahydrothieno[2,3-c]pyridine scaffold. Among these compounds, compound 9b and 10b showed excellent antagonistic activity in vitro and demonstrated pain-suppressing activity in animal models of pain. Both compounds were orally active, and compound 9b exhibited a favorable pharmacokinetic profile in rats. We believe that these compounds can provide a promising lead compound that is suitable for the potential treatment of neuropathic pain.
URI
http://pubs.kist.re.kr/handle/201004/49842
ISSN
02235234
Appears in Collections:
KIST Publication > Article
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