Discovery of 2-(1H-indazol-1-yl)-thiazole derivatives as selective EP1 receptor antagonists for treatment of overactive bladder by core structure replacement
We have designed a series of potent EP1 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...
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| Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2014-03, Vol.24 (5), p.1327-1333 |
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| container_end_page | 1333 |
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| container_issue | 5 |
| container_start_page | 1327 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 24 |
| creator | Atobe, Masakazu Naganuma, Kenji Kawanishi, Masashi Morimoto, Akifumi Kasahara, Ken-ichi Ohashi, Shigeki Suzuki, Hiroko Hayashi, Takahiko Miyoshi, Shiro |
| description | We have designed a series of potent EP1 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 compound and further optimization of this series promises to provide a novel class of drug for treating overactive bladder (OAB). |
| doi_str_mv | 10.1016/j.bmcl.2014.01.052 |
| format | Article |
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| ispartof | Bioorganic & medicinal chemistry letters, 2014-03, Vol.24 (5), p.1327-1333 |
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| language | eng |
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| source | Elsevier ScienceDirect Journals Complete |
| title | Discovery of 2-(1H-indazol-1-yl)-thiazole derivatives as selective EP1 receptor antagonists for treatment of overactive bladder by core structure replacement |
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