- 3-Urea-1-(phenylmethyl)-pyridones as novel, potent, and selective EP 3 receptor antagonists
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A series of 3-urea-1-(phenylmethyl)-pyridones was discovered as novel EP3 antagonists via high-throughput screening and subsequent optimization. The synthesis, structure-activity relationships, and optimization of the initial hit that resulted in potent and selective EP3 receptor antagonists such as 11g are described.
- Li, Yue H.,Tseng, Pei-San,Evans, Karen A.,Jaworski, Jon-Paul,Morrow, Dwight M.,Fries, Harvey E.,Wu, Charlene W.,Edwards, Richard M.,Jin, Jian
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scheme or table
p. 6744 - 6747
(2010/12/20)
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- Oligocyclization of 2-(hydroxymethyl)pyrroles with electron-withdrawing groups at β-positions: Formation and structural elucidation of porphyrinogens and hexaphyrinogens
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Acid-catalyzed oligomerization of 2-(hydroxymethyl)pyrroles bearing C6F5, 2,6-Cl2C6H3, CF3 and CO2Et groups at β-positions was examined. The reaction of ethyl pyrrole-3-carboxylates gave a mixture of oligomers and type I isomers of porphyrinogens and hexaphyrinogens were isolated when the other β-substituents were sufficiently bulky, for example, mesityl, 2,6-Cl2C6H3 and C6F5 groups. On the other hand, the pyrroles having other electron-withdrawing groups afforded porphyrinogens as the only isolable products.
- Uno, Hidemitsu,Inoue, Kentarou,Inoue, Takashi,Ono, Noboru
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p. 3857 - 3865
(2007/10/03)
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- Preparation of novel heteroisoindoles from nitropyridines and nitropyridones
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The reaction of nitropyridine derivatives with ethyl isocyanoacetate in the presence of 1,8-diazabicyclo[5.4.0]undecene proceeded tandem cyclization to give polycyclic pyrrolopyridines or imidazopyridines. On the other hand, N-protected 3-nitro- and 5-nitropyridones and N,N-diprotected 5-nitrouracil gave corresponding bicyclic pyrroles in good yields under the similar conditions.
- Murashima, Takashi,Nishi, Keiji,Nakamoto, Ken-ichi,Kato, Atsushi,Tamai, Ryuji,Uno, Hidemitsu,Ono, Noboru
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p. 301 - 310
(2007/10/03)
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- Nonpeptidic, monocharged, cell permeable ligands for the p56lck SH2 domain
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p56lck is a member of the src family of tyrosine kinases and plays a critical role in the signal transduction events that lead to T cell activation. Ligands for the p56lck SH2 domain have the potential to disrupt the interaction of p56lck with its substra
- Proudfoot,Betageri,Cardozo,Gilmore,Glynn,Hickey,Jakes,Kabcenell,Kirrane,Tibolla,Lukas,Patel,Sharma,Yazdanian,Moss,Beaulieu,Cameron,Ferland,Gauthier,Gillard,Gorys,Poirier,Rancourt,Wernic,Montse
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p. 2421 - 2431
(2007/10/03)
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