Thienopyrrole acetic acids as antagonists of the CRTH2 receptor

Dominique Bonafoux; Ayome Abibi; Brian Bettencourt; Andrew Burchat; Anna Ericsson; Christopher M Harris; Tegest Kebede; Michael Morytko; Michael McPherson; Grier Wallace; Xiaoyun Wu

doi:10.1016/j.bmcl.2011.01.008

Thienopyrrole acetic acids as antagonists of the CRTH2 receptor

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1861-4. doi: 10.1016/j.bmcl.2011.01.008. Epub 2011 Jan 14.

Authors

Dominique Bonafoux¹, Ayome Abibi, Brian Bettencourt, Andrew Burchat, Anna Ericsson, Christopher M Harris, Tegest Kebede, Michael Morytko, Michael McPherson, Grier Wallace, Xiaoyun Wu

Affiliation

¹ Abbott Laboratories, Worcester, MA 01605, USA. dominique.bonafoux@abbott.com

PMID: 21316222
DOI: 10.1016/j.bmcl.2011.01.008

Abstract

The bioisosteric replacement of the indole core of CRTH2 antagonists using thienopyrroles was investigated, resulting in potent antagonists with good selectivity over DP1. Early ADME/PK assessment of this chemotype demonstrated bioavailability in mice.

MeSH terms

Acetates / chemistry
Acetates / pharmacokinetics
Acetates / pharmacology*
Animals
Biological Availability
Mice
Microsomes, Liver / metabolism
Pyrroles / chemistry*
Rats
Receptors, Immunologic / antagonists & inhibitors*
Receptors, Prostaglandin / antagonists & inhibitors*

Substances

Acetates
Pyrroles
Receptors, Immunologic
Receptors, Prostaglandin
thienopyrrole
prostaglandin D2 receptor