Novel methylene-linked heterocyclic EP1 receptor antagonists.
We describe the SAR, in terms of heterocyclic replacements, for a series of pyrazole EP(1) receptor antagonists. This study led to the identification of several aromatic heterocyclic replacements for the pyrazole in the original compound. Investigation of replacements for the methylene linker uncovered disparate SAR in the thiazole and pyridine series.
Hall
Adrian
A
Neurology Centre of Excellence for Drug Discovery, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, United Kingdom. adrian.2.hall@gsk.com
Bit
Rino A
RA
Brown
Susan H
SH
Chowdhury
Anita
A
Giblin
Gerard M P
GM
Hurst
David N
DN
Kilford
Ian R
IR
Lewell
Xiao
X
Naylor
Alan
A
Scoccitti
Tiziana
T
D006571:Heterocyclic Compounds / Q000737:chemistry* / Q000494:pharmacology*; D008958:Models, Molecular; D015394:Molecular Structure; D011485:Protein Binding; D018078:Receptors, Prostaglandin E / Q000037:antagonists & inhibitors*; D058306:Receptors, Prostaglandin E, EP1 Subtype; D013329:Structure-Activity Relationship
D006571:Heterocyclic Compounds; D018078:Receptors, Prostaglandin E; D058306:Receptors, Prostaglandin E, EP1 Subtype