New class of biphenylene dibenzazocinones as potent ligands for the human EP1 prostanoid receptor.
A new class of potent and selective ligands for the human EP1 prostanoid receptor is described. SAR studies reported herein allowed the identification of several potent dibenzazocinones bearing an acylsulfonamide side chain. The binding affinity of these compounds on all eight human prostanoid receptors is reported.
Ruel
R
R
Merck Frosst Centre for Therapeutic Research, Pointe Claire - Dorval, Québec, Canada.
Lacombe
P
P
Abramovitz
M
M
Godbout
C
C
Lamontagne
S
S
Rochette
C
C
Sawyer
N
N
Stocco
R
R
Tremblay
N M
NM
Metters
K M
KM
Labelle
M
M
D001392:Azocines / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D001713:Biphenyl Compounds / Q000737:chemistry / Q000378:metabolism / Q000494:pharmacology*; D006801:Humans; D008024:Ligands; D011485:Protein Binding; D018078:Receptors, Prostaglandin E / Q000187:drug effects* / Q000378:metabolism; D058306:Receptors, Prostaglandin E, EP1 Subtype; D013329:Structure-Activity Relationship
D001392:Azocines; D001713:Biphenyl Compounds; D008024:Ligands; C545635:PTGER1 protein, human; D018078:Receptors, Prostaglandin E; D058306:Receptors, Prostaglandin E, EP1 Subtype