Structure–Activity Relationship of Biaryl Acylsulfonamide Analogues on the Human EP3 Prostanoid Receptor

https://doi.org/10.1016/S0960-894X(02)00518-8Get rights and content

Abstract

Potent and selective ligands for the human EP3 prostanoid receptor are described. Biaryl compounds bearing a tethered ortho substituted acidic moiety were identified as potent EP3 antagonists based on the SAR described herein. The binding affinity of key compounds on all eight human prostanoid receptors is reported.

Potent and selective ligands for the human EP3 prostanoid receptor are described. Biaryl compounds bearing a tethered ortho substituted acidic moiety were identified as potent EP3 antagonists based on the SAR described herein. The binding affinity of key compounds on all eight human prostanoid receptors is reported.

  1. Download : Download full-size image

Section snippets

Acknowledgements

The authors would like to thank Dr Daniel Dubé for proofreading this manuscript.

References (12)

  • Y. Sugimoto et al.

    Prog. Lipid. Res.

    (2000)
    S. Narumiya et al.

    Physiol. Rev.

    (1999)
    R.A. Coleman et al.

    Pharmacol. Rev.

    (1994)
  • W.T. Ashton et al.

    J. Med. Chem.

    (1994)
  • R.W. Friesen et al.

    Tetrahedron Lett.

    (1993)
  • M. Abramovitz et al.

    Biochim. Biophys. Acta

    (2000)
  • A. Kiryiama et al.

    Br. J. Pharmacol.

    (1997)
  • Y. Shimazaki et al.

    Bioorg. Med. Chem.

    (2000)
There are more references available in the full text version of this article.

Cited by (39)

View all citing articles on Scopus
View full text