title: Thienopyrrole acetic acids as antagonists of the CRTH2 receptor.
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.
authors.affiliation: Abbott Laboratories, Worcester, MA 01605, USA. dominique.bonafoux@abbott.com
authors.forename: Dominique
authors.initials: D
authors.lastname: Bonafoux
authors.forename: Ayome
authors.initials: A
authors.lastname: Abibi
authors.forename: Brian
authors.initials: B
authors.lastname: Bettencourt
authors.forename: Andrew
authors.initials: A
authors.lastname: Burchat
authors.forename: Anna
authors.initials: A
authors.lastname: Ericsson
authors.forename: Christopher M
authors.initials: CM
authors.lastname: Harris
authors.forename: Tegest
authors.initials: T
authors.lastname: Kebede
authors.forename: Michael
authors.initials: M
authors.lastname: Morytko
authors.forename: Michael
authors.initials: M
authors.lastname: McPherson
authors.forename: Grier
authors.initials: G
authors.lastname: Wallace
authors.forename: Xiaoyun
authors.initials: X
authors.lastname: Wu
mesh_terms: D000085:Acetates / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology*; D000818:Animals; D001682:Biological Availability; D051379:Mice; D008862:Microsomes, Liver / Q000378:metabolism; D011758:Pyrroles / Q000737:chemistry*; D051381:Rats; D011971:Receptors, Immunologic / Q000037:antagonists & inhibitors*; D011982:Receptors, Prostaglandin / Q000037:antagonists & inhibitors*
chemical_list: D000085:Acetates; D011758:Pyrroles; D011971:Receptors, Immunologic; D011982:Receptors, Prostaglandin; C521801:thienopyrrole; C036293:prostaglandin D2 receptor