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…

Index: 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

Full Text: HTML

Citation Number: 8

Abstract

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 ...

Related Articles:

Synthesis of Substituted 1 H-Indazoles from Arynes and Hydrazones

[Li, Pan; Wu, Chunrui; Zhao, Jingjing; Rogness, Donald C.; Shi, Feng Journal of Organic Chemistry, 2012 , vol. 77, # 7 p. 3149 - 3158]

ML212: A small-molecule probe for investigating fluconazole resistance mechanisms in Candida albicans

[Youngsaye, Willmen; Hartland, Cathy L.; Morgan, Barbara J.; Ting, Amal; Nag, Partha P.; Vincent, Benjamin; Mosher, Carrie A.; Bittker, Joshua A.; Dandapani, Sivaraman; Palmer, Michelle; Whitesell, Luke; Lindquist, Susan; Schreiber, Stuart L.; Munoz, Benito Beilstein Journal of Organic Chemistry, 2013 , vol. 9, p. 1501 - 1507]

Synthesis of 3-substituted indazoles from arynes and N-tosylhydrazones

[Li, Pan; Zhao, Jingjing; Wu, Chunrui; Larock, Richard C.; Shi, Feng Organic Letters, 2011 , vol. 13, # 13 p. 3340 - 3343]

Synthesis of 3-substituted indazoles from arynes and N-tosylhydrazones

[Li, Pan; Zhao, Jingjing; Wu, Chunrui; Larock, Richard C.; Shi, Feng Organic Letters, 2011 , vol. 13, # 13 p. 3340 - 3343]

RhIII/CuII-Cocatalyzed Synthesis of 1 H-Indazoles through C–H Amidation and N–N Bond Formation

[Yu, Da-Gang; Suri, Mamta; Glorius, Frank Journal of the American Chemical Society, 2013 , vol. 135, # 24 p. 8802 - 8805]

More Articles...