SAR-based optimization of 2-(1H-pyrazol-1-yl)-thiazole derivatives as highly potent EP 1 receptor antagonists

…, A Morimoto, K Kasahara, S Ohashi, H Suzuki…

文献索引：Atobe, Masakazu; Naganuma, Kenji; Kawanishi, Masashi; Morimoto, Akifumi; Kasahara, Ken-Ichi; Ohashi, Shigeki; Suzuki, Hiroko; Hayashi, Takahiko; Miyoshi, Shiro Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 24 p. 6569 - 6576

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被引用次数: 9

摘要

Abstract We describe a medicinal chemistry approach for generating a series of 2-(1H- pyrazol-1-yl) thiazoles as EP 1 receptor antagonists. To improve the physicochemical properties of compound 1, we investigated its structure–activity relationships (SAR). Optimization of this lead compound provided small compound 25 which exhibited the best EP 1 receptor antagonist activity and a good SAR profile.