Discovery of novel biaryl heterocyclic EP1 receptor antagonists

Adrian Hall; Rino A Bit; Susan H Brown; Helene M Chaignot; Iain P Chessell; Tanya Coleman; Gerard M P Giblin; David N Hurst; Ian R Kilford; Xiao Q Lewell; Anton D Michel; Shiyam Mohamed; Alan Naylor; Riccardo Novelli; Lee Skinner; David J Spalding; Sac P Tang; Richard J Wilson

doi:10.1016/j.bmcl.2006.02.014

Discovery of novel biaryl heterocyclic EP1 receptor antagonists

Bioorg Med Chem Lett. 2006 May 15;16(10):2666-71. doi: 10.1016/j.bmcl.2006.02.014. Epub 2006 Feb 28.

Authors

Adrian Hall¹, Rino A Bit, Susan H Brown, Helene M Chaignot, Iain P Chessell, Tanya Coleman, Gerard M P Giblin, David N Hurst, Ian R Kilford, Xiao Q Lewell, Anton D Michel, Shiyam Mohamed, Alan Naylor, Riccardo Novelli, Lee Skinner, David J Spalding, Sac P Tang, Richard J Wilson

Affiliation

¹ Neurology and Gastrointestinal Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. [email protected]

PMID: 16503138
DOI: 10.1016/j.bmcl.2006.02.014

Abstract

We describe the generation of novel EP(1) receptor antagonists by investigation of thiophene isosteres. In addition, we disclose preliminary in vitro and in vivo DMPK for selected compounds.

MeSH terms

Animals
Heterocyclic Compounds / chemistry*
Heterocyclic Compounds / pharmacology*
In Vitro Techniques
Rats
Receptors, Prostaglandin E / antagonists & inhibitors*
Receptors, Prostaglandin E, EP1 Subtype

Substances

Heterocyclic Compounds
Receptors, Prostaglandin E
Receptors, Prostaglandin E, EP1 Subtype