Discovery of a novel series of nonacidic benzofuran EP1 receptor antagonists

Amanda C Allan; Andy Billinton; Susan H Brown; Anita Chowdhury; Andrew J Eatherton; Charlotte Fieldhouse; Gerard M P Giblin; Paul Goldsmith; Adrian Hall; David N Hurst; Alan Naylor; D Anthony Rawlings; Mairi Sime; Tiziana Scoccitti; Pamela J Theobald

doi:10.1016/j.bmcl.2011.05.047

Discovery of a novel series of nonacidic benzofuran EP1 receptor antagonists

Bioorg Med Chem Lett. 2011 Jul 15;21(14):4343-8. doi: 10.1016/j.bmcl.2011.05.047. Epub 2011 May 23.

Authors

Amanda C Allan¹, Andy Billinton, Susan H Brown, Anita Chowdhury, Andrew J Eatherton, Charlotte Fieldhouse, Gerard M P Giblin, Paul Goldsmith, Adrian Hall, David N Hurst, Alan Naylor, D Anthony Rawlings, Mairi Sime, Tiziana Scoccitti, Pamela J Theobald

Affiliation

¹ Neurosciences Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom.

PMID: 21676612
DOI: 10.1016/j.bmcl.2011.05.047

Abstract

We describe the discovery and optimization of a novel series of benzofuran EP(1) antagonists, leading to the identification of 26d, a novel nonacidic EP(1) antagonist which demonstrated efficacy in preclinical models of chronic inflammatory pain.

MeSH terms

Animals
Anti-Inflammatory Agents, Non-Steroidal / chemistry*
Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
Anti-Inflammatory Agents, Non-Steroidal / therapeutic use
Benzofurans / chemistry*
Benzofurans / pharmacokinetics
Benzofurans / therapeutic use
Cell Line
Disease Models, Animal
Dogs
Drug Evaluation, Preclinical
Pain / drug therapy
Rats
Receptors, Prostaglandin E, EP1 Subtype / antagonists & inhibitors*
Receptors, Prostaglandin E, EP1 Subtype / metabolism
Structure-Activity Relationship

Substances

Anti-Inflammatory Agents, Non-Steroidal
Benzofurans
Receptors, Prostaglandin E, EP1 Subtype
benzofuran