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Novel thienopyrimidinones as mGluR1 antagonists

Authors
Kim, YoungjaeKim, JeeyeonKim, SoraKi, YooranSeo, Seon HeeTae, JinsungKo, Min KyungJang, Hyun-SeoLim, Eun JeongSong, ChimanCho, YoonJeongKoh, Hae-YoungChong, YouhoonChoo, Il HanKeum, GyochangMin, Sun-JoonChoo, Hyunah
Issue Date
Oct-2014
Publisher
Elsevier BV
Keywords
mGluR1 antagonist; Thienopyrimidinone; CNS disease; Glutamate; Metabotropic
Citation
European Journal of Medicinal Chemistry, v.85, pp.629 - 637
Indexed
SCIE
SCOPUS
Journal Title
European Journal of Medicinal Chemistry
Volume
85
Start Page
629
End Page
637
URI
https://scholarworks.bwise.kr/erica/handle/2021.sw.erica/21541
DOI
10.1016/j.ejmech.2014.08.027
ISSN
0223-5234
Abstract
There has been much attention to discover mGluR1 antagonists for treating various central nervous system diseases such as seizures and neuropathic pain. Thienopyrimidinone derivatives were designed, synthesized, and biologically evaluated against mGluR1. Among the synthesized compounds, 3-(4-methoxyphenyl)-7-(o-tolyl)thienopyrimidin-4-one 30 exhibited the most potent inhibitory activity with an IC50 value of 45 nM and good selectivity over mGluR5. Also, the selective mGluR1 antagonist 30 showed marginal hERG channel activity (IC50 = 9.87 mu M), good profiles to CYP isozymes, and a good pharmacokinetic profile. Overall, the compound 30 was identified as a selective mGluR1 antagonist with a good pharmacokinetic profile, which is probably devoid of cardiac side effect and drug drug interactions. Therefore, the compound 30 can be expected to be broadly used as mGluR1 antagonistic chemical probe in in vitro and in vivo study for investigating CNS diseases. (C) 2014 Elsevier Masson SAS. All rights reserved.
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COLLEGE OF SCIENCE AND CONVERGENCE TECHNOLOGY (DEPARTMENT OF CHEMICAL AND MOLECULAR ENGINEERING)
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