3-Indolyl sultams as selective CRTh2 antagonists.
CRTh2 (DP(2)) is a prostaglandin D(2) receptor implicated in the recruitment of eosinophils and basophils within the asthmatic lung. Here we report the discovery of a novel series of 3-indolyl sultam antagonists with low nM affinity for CRTh2. These compounds proved to be selective over the other primary prostaglandin D(2) receptor (DP1) as well as the thromboxane A(2) receptor (TP).
Tumey
L Nathan
LN
Athersys, Inc., 3201 Carnegie Ave., Cleveland, OH 44115, USA. tumeyn@wyeth.com
Robarge
Michael J
MJ
Gleason
Elizabeth
E
Song
Jianping
J
Murphy
Steven M
SM
Ekema
George
G
Doucette
Chris
C
Hanniford
Doug
D
Palmer
Marc
M
Pawlowski
Gary
G
Danzig
Joel
J
Loftus
Margaret
M
Hunady
Karen
K
Sherf
Bruce
B
Mays
Robert W
RW
Stricker-Krongrad
Alain
A
Brunden
Kurt R
KR
Bennani
Youssef L
YL
Harrington
John J
JJ
D004951:Esterification; D006801:Humans; D007211:Indoles / Q000737:chemistry* / Q000494:pharmacology*; D011971:Receptors, Immunologic / Q000037:antagonists & inhibitors*; D011982:Receptors, Prostaglandin / Q000037:antagonists & inhibitors*; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology*
D007211:Indoles; D011971:Receptors, Immunologic; D011982:Receptors, Prostaglandin; D013449:Sulfonamides; C036293:prostaglandin D2 receptor