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 …

…, T Nagase, M Tanaka, Y Yamaura, H Takizawa…

Index: Asada, Masaki; Iwahashi, Maki; Obitsu, Tetsuo; Kinoshita, Atsushi; Nakai, Yoshihiko; Onoda, Takahiro; Nagase, Toshihiko; Tanaka, Motoyuki; Yamaura, Yoshiyuki; Takizawa, Hiroya; Yoshikawa, Ken; Sato, Kazutoyo; Narita, Masami; Ohuchida, Shuichi; Nakai, Hisao; Toda, Masaaki Bioorganic and Medicinal Chemistry, 2010 , vol. 18, # 4 p. 1641 - 1658

Full Text: HTML

Citation Number: 9

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- ...