| Literature DB >> 20346663 |
Masaki Asada1, Tetsuo Obitsu, Atsushi Kinoshita, Yoshihiko Nakai, Toshihiko Nagase, Isamu Sugimoto, Motoyuki Tanaka, Hiroya Takizawa, Ken Yoshikawa, Kazutoyo Sato, Masami Narita, Shuichi Ohuchida, Hisao Nakai, Masaaki Toda.
Abstract
A series of novel N-acylsulfonamide analogs were synthesized and evaluated for their binding affinity and antagonist activity for the EP3 receptor subtype. Representative compounds were also evaluated for their inhibitory effect on PGE(2)-induced uterine contraction in pregnant rats. Among those tested, a series of N-acylbenzenesulfonamide analogs were found to be more potent than the corresponding carboxylic acid analogs in both the in vitro and in vivo evaluations. The structure activity relationships (SAR) are also discussed. Copyright 2010. Published by Elsevier Ltd.Entities:
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Year: 2010 PMID： 20346663 DOI： 10.1016/j.bmcl.2010.02.034
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823