1233249-57-4Relevant academic research and scientific papers
Isoquinoline derivatives as potent CRTH2 receptor antagonists: Synthesis and SAR
Nishikawa-Shimono, Rie,Sekiguchi, Yoshinori,Koami, Takeshi,Kawamura, Madoka,Wakasugi, Daisuke,Watanabe, Kazuhito,Wakahara, Shunichi,Matsumoto, Kayo,Takayama, Tetsuo
, p. 3305 - 3310 (2012/06/18)
Synthesis and structure-activity relationship of a novel series of isoquinoline CRTH2 receptor antagonists are described. One of the most potent compounds, TASP0376377 (6m), showed not only potent binding affinity (IC 50 = 19 nM) but also excellent functional antagonist activity (IC50 = 13 nM). TASP0376377 was tested for its ability of a chemotaxis assay to show the effectiveness (IC50 = 23 nM), which was in good agreement with the CRTH2 antagonist potency. Furthermore, TASP0376377 showed sufficient selectivity for binding to CRTH2 over the DP1 prostanoid receptor (IC50 >1 μM) and COX-1 and COX-2 enzymes (IC 50 >10 μM).
ISOQUINOLINE DERIVATIVE
-
Page/Page column 44, (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.
