Structure-activity relationship on the human EP3 prostanoid receptor by use of solid-support chemistry.
Potent and selective EP3 receptor ligands were found by making a library using solid-support chemistry. These compounds can be obtained by a Suzuki coupling reaction of a solid-supported benzyl bromide using various boronic acids. The yields obtained for this reaction were in the range of 24-95% of arylmethyl cinnamic acid 1 after cleavage from the Wang resin.
Merck Frosst Canada & Co., Pointe-Claire, Dorval, Québec. helene_juteau@merck.com
H
H
Juteau
Y
Y
Gareau
M
M
Labelle
S
S
Lamontagne
N
N
Tremblay
M C
MC
Carrière
N
N
Sawyer
D
D
Denis
K M
KM
Metters
D002934:Cinnamates / Q000138:chemical synthesis* / Q000737:chemistry / Q000378:metabolism* / Q000494:pharmacology; D020650:Combinatorial Chemistry Techniques; D006801:Humans; D008024:Ligands; D015394:Molecular Structure; D018078:Receptors, Prostaglandin E / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism*; D058308:Receptors, Prostaglandin E, EP3 Subtype; D013329:Structure-Activity Relationship
D002934:Cinnamates; D008024:Ligands; C545647:PTGER3 protein, human; D018078:Receptors, Prostaglandin E; D058308:Receptors, Prostaglandin E, EP3 Subtype; C029010:cinnamic acid