Title of article :
3-(2-Aminocarbonylphenyl)propanoic acid analogs as potent and selective EP3 receptor antagonists. Part 2: Optimization of the side chains to improve in vitro and in vivo potencies Original Research Article
Author/Authors :
Masaki Asada، نويسنده , , Maki Iwahashi، نويسنده , , Tetsuo Obitsu، نويسنده , , Atsushi Kinoshita، نويسنده , , Yoshihiko Nakai، نويسنده , , Takahiro Onoda، نويسنده , , Toshihiko Nagase، نويسنده , , Motoyuki Tanaka، نويسنده , , Yoshiyuki Yamaura، نويسنده , , Hiroya Takizawa، نويسنده , , Ken Yoshikawa، نويسنده , , Kazutoyo Sato، نويسنده , , Masami Narita، نويسنده , , Shuichi Ohuchida، نويسنده , , Hisao Nakai، نويسنده , , Masaaki Toda، نويسنده ,
Issue Information :
روزنامه با شماره پیاپی سال 2010
Pages :
18
From page :
1641
To page :
1658
Abstract :
A series of 3-[2-{[(3-methyl-1-phenylbutyl)amino]carbonyl}-4-(phenoxymethyl)phenyl]propanoic acid analogs were synthesized and evaluated for their in vitro potency. In most cases, introduction of one or two substituents into the two phenyl moieties resulted in the tendency of an increase or retention of in vitro activities. Several compounds, which showed excellent subtype selectivity, were evaluated for their inhibitory effect against PGE2-induced uterine contraction in pregnant rats, which is thought to be mediated by the EP3 receptor subtype. The structure–activity relationships (SARs) are also discussed.
Keywords :
Antagonist , EP3 receptor , Uterine contraction
Journal title :
Bioorganic and Medicinal Chemistry
Serial Year :
2010
Journal title :
Bioorganic and Medicinal Chemistry
Record number :
1307166
Link To Document :
بازگشت