Discovery of novel biaryl heterocyclic EP1 receptor antagonists.
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.
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
Bit
Rino A
RA
Brown
Susan H
SH
Chaignot
Helene M
HM
Chessell
Iain P
IP
Coleman
Tanya
T
Giblin
Gerard M P
GM
Hurst
David N
DN
Kilford
Ian R
IR
Lewell
Xiao Q
XQ
Michel
Anton D
AD
Mohamed
Shiyam
S
Naylor
Alan
A
Novelli
Riccardo
R
Skinner
Lee
L
Spalding
David J
DJ
Tang
Sac P
SP
Wilson
Richard J
RJ
D000818:Animals; D006571:Heterocyclic Compounds / Q000737:chemistry* / Q000494:pharmacology*; D066298:In Vitro Techniques; D051381:Rats; D018078:Receptors, Prostaglandin E / Q000037:antagonists & inhibitors*; D058306:Receptors, Prostaglandin E, EP1 Subtype
D006571:Heterocyclic Compounds; D018078:Receptors, Prostaglandin E; D058306:Receptors, Prostaglandin E, EP1 Subtype