Discovery of novel, non-acidic 1,5-biaryl pyrrole EP1 receptor antagonists

Adrian Hall; Stephen Atkinson; Susan H Brown; Iain P Chessell; Anita Chowdhury; Gerard M P Giblin; Paul Goldsmith; Mark P Healy; Karamjit S Jandu; Matthew R Johnson; Anton D Michel; Alan Naylor; Jennifer A Sweeting

doi:10.1016/j.bmcl.2006.12.021

Discovery of novel, non-acidic 1,5-biaryl pyrrole EP1 receptor antagonists

Bioorg Med Chem Lett. 2007 Mar 1;17(5):1200-5. doi: 10.1016/j.bmcl.2006.12.021. Epub 2006 Dec 12.

Authors

Adrian Hall¹, Stephen Atkinson, Susan H Brown, Iain P Chessell, Anita Chowdhury, Gerard M P Giblin, Paul Goldsmith, Mark P Healy, Karamjit S Jandu, Matthew R Johnson, Anton D Michel, Alan Naylor, Jennifer A Sweeting

Affiliation

¹ Neurology and Gastrointestinal Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. adrian.2.hall@gsk.com

PMID: 17196385
DOI: 10.1016/j.bmcl.2006.12.021

Abstract

Replacement of the carboxylic acid group in a series of previously described 1,5-biaryl pyrrole EP1 receptor antagonists led to the discovery of various novel non-acidic antagonists. Several analogues displayed high binding affinity and high binding efficiency indices.

MeSH terms

Humans
Inhibitory Concentration 50
Protein Binding
Pyrroles / chemistry*
Pyrroles / pharmacology*
Receptors, Prostaglandin E / antagonists & inhibitors*
Receptors, Prostaglandin E, EP1 Subtype
Structure-Activity Relationship

Substances

PTGER1 protein, human
Pyrroles
Receptors, Prostaglandin E
Receptors, Prostaglandin E, EP1 Subtype