Discovery of 2-(1H-indazol-1-yl)-thiazole derivatives as selective EP 1 receptor antagonists for treatment of overactive bladder by core structure replacement

…, 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, 2014 , vol. 24, # 5 p. 1327 - 1333

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被引用次数: 8

摘要

Abstract We have designed a series of potent EP 1 receptor antagonists. These antagonists are a series of 2-(1H-indazol-1-yl)-thiazoles in which the core structure was replaced with pyrazole-phenyl groups. In preliminary conscious rat cystometry experiments, two representative candidates, 2 and 22, increased bladder capacity. In particular, the increase using 22 was approximately 2-fold that of the baseline. More detailed profiling of this ...