Discovery of novel, non-acidic 1,5-biaryl pyrrole EP1 receptor antagonists.
Replacement of the carboxylic acid group in a series of previously described 1,5-biaryl pyrrole EP1 receptor antagonists led to the discovery of various novel non-acidic antagonists. Several analogues displayed high binding affinity and high binding efficiency indices.
Hall
Adrian
A
Neurology and Gastrointestinal Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. adrian.2.hall@gsk.com
Atkinson
Stephen
S
Brown
Susan H
SH
Chessell
Iain P
IP
Chowdhury
Anita
A
Giblin
Gerard M P
GM
Goldsmith
Paul
P
Healy
Mark P
MP
Jandu
Karamjit S
KS
Johnson
Matthew R
MR
Michel
Anton D
AD
Naylor
Alan
A
Sweeting
Jennifer A
JA
D006801:Humans; D020128:Inhibitory Concentration 50; D011485:Protein Binding; D011758:Pyrroles / Q000737:chemistry* / Q000494:pharmacology*; D018078:Receptors, Prostaglandin E / Q000037:antagonists & inhibitors*; D058306:Receptors, Prostaglandin E, EP1 Subtype; D013329:Structure-Activity Relationship
C545635:PTGER1 protein, human; D011758:Pyrroles; D018078:Receptors, Prostaglandin E; D058306:Receptors, Prostaglandin E, EP1 Subtype