1233248-10-6Relevant articles and documents
Isoquinoline derivatives as potent CRTH2 antagonists: Design, synthesis and SAR
Nishikawa-Shimono, Rie,Sekiguchi, Yoshinori,Koami, Takeshi,Kawamura, Madoka,Wakasugi, Daisuke,Watanabe, Kazuhito,Wakahara, Shunichi,Kimura, Kayo,Yamanobe, Susumu,Takayama, Tetsuo
, p. 7674 - 7685 (2014/01/06)
In this study, we describe the synthesis and structure-activity relationship (SAR) of a series of isoquinoline chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2) antagonists. TASP0376377 (15-20), one of the most potent compounds, showed a potent binding affinity (IC50 = 19 nM) in addition to the excellent functional antagonist activity (IC50 = 13 nM). Moreover, the efficacy of this compound in a chemotaxis assay (IC50 = 23 nM) was in good agreement with its potency as a CRTH2 antagonist. In addition, 15-20 exhibited greater selectivity in binding to CRTH2 than to the DP1 prostanoid receptor (IC 50 >1 μM) or the enzymes COX-1 and COX-2 (IC50 >10 μM).
ISOQUINOLINE DERIVATIVE
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Page/Page column 42, (2011/11/01)
A compound represented by formula (I) or a pharmaceutically acceptable salt thereof has an effect of inhibiting CRTH2 and, therefore, is useful as a preventive or a remedy for allergic diseases such as asthma, atopic dermatitis and allergic rhinitis.