New class of biphenylene dibenzazocinones as potent ligands for the human EP1 prostanoid receptor

R Ruel; P Lacombe; M Abramovitz; C Godbout; S Lamontagne; C Rochette; N Sawyer; R Stocco; N M Tremblay; K M Metters; M Labelle

doi:10.1016/s0960-894x(99)00465-5

New class of biphenylene dibenzazocinones as potent ligands for the human EP1 prostanoid receptor

Bioorg Med Chem Lett. 1999 Sep 20;9(18):2699-704. doi: 10.1016/s0960-894x(99)00465-5.

Authors

R Ruel¹, P Lacombe, M Abramovitz, C Godbout, S Lamontagne, C Rochette, N Sawyer, R Stocco, N M Tremblay, K M Metters, M Labelle

Affiliation

¹ Merck Frosst Centre for Therapeutic Research, Pointe Claire - Dorval, Québec, Canada.

PMID: 10509919
DOI: 10.1016/s0960-894x(99)00465-5

Abstract

A new class of potent and selective ligands for the human EP1 prostanoid receptor is described. SAR studies reported herein allowed the identification of several potent dibenzazocinones bearing an acylsulfonamide side chain. The binding affinity of these compounds on all eight human prostanoid receptors is reported.

MeSH terms

Azocines / chemistry
Azocines / metabolism
Azocines / pharmacology*
Biphenyl Compounds / chemistry
Biphenyl Compounds / metabolism
Biphenyl Compounds / pharmacology*
Humans
Ligands
Protein Binding
Receptors, Prostaglandin E / drug effects*
Receptors, Prostaglandin E / metabolism
Receptors, Prostaglandin E, EP1 Subtype
Structure-Activity Relationship

Substances

Azocines
Biphenyl Compounds
Ligands
PTGER1 protein, human
Receptors, Prostaglandin E
Receptors, Prostaglandin E, EP1 Subtype