Structure-activity relationship of cinnamic acylsulfonamide analogues on the human EP3 prostanoid receptor

Potent and selective antagonists of the human EP3 receptor have been identified. The structure-activity relationship of the chemical series was conducted and we found several analogues displaying sub-nanomolar K(i) values at the EP3 receptor and micromolar activities at the EP1, EP2 and EP4 receptor...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry 2001-08, Vol.9 (8), p.1977-1984
Main Authors: JUTEAU, Hélène, GAREAU, Yves, LABELLE, Marc, STURINO, Claudio F, SAWYER, Nicole, TREMBLAY, Nathalie, LAMONTAGNE, Sonia, CARRIERE, Marie-Claude, DENIS, Danielle, METTERS, Kathleen M
Format: Article
Language:English
Subjects:
Biological and medical sciences
Cinnamates - chemistry
Cinnamates - pharmacology
Humans
Medical sciences
Miscellaneous
Pharmacology. Drug treatments
Prostaglandin Antagonists - chemistry
Prostaglandin Antagonists - pharmacology
Receptors, Prostaglandin E - drug effects
Receptors, Prostaglandin E - metabolism
Receptors, Prostaglandin E, EP3 Subtype
Structure-Activity Relationship
Sulfonamides - chemistry
Sulfonamides - pharmacology
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Summary:Potent and selective antagonists of the human EP3 receptor have been identified. The structure-activity relationship of the chemical series was conducted and we found several analogues displaying sub-nanomolar K(i) values at the EP3 receptor and micromolar activities at the EP1, EP2 and EP4 receptors. The effect of added human serum albumin (HSA) on the binding affinity at the EP3 receptor was also investigated.
ISSN:0968-0896
1464-3391
DOI:10.1016/S0968-0896(01)00110-9