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

H Juteau; Y Gareau; M Labelle; C F Sturino; N Sawyer; N Tremblay; S Lamontagne; M C Carrière; D Denis; K M Metters

doi:10.1016/s0968-0896(01)00110-9

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

Bioorg Med Chem. 2001 Aug;9(8):1977-84. doi: 10.1016/s0968-0896(01)00110-9.

Authors

H Juteau¹, Y Gareau, M Labelle, C F Sturino, N Sawyer, N Tremblay, S Lamontagne, M C Carrière, D Denis, K M Metters

Affiliation

¹ Merck Frosst Canada & Co., Pointe-Claire-Dorval, H9R 4P8, Québec, Canada.

PMID: 11504634
DOI: 10.1016/s0968-0896(01)00110-9

Abstract

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.

MeSH terms

Cinnamates / chemistry
Cinnamates / pharmacology*
Humans
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*

Substances

Cinnamates
PTGER3 protein, human
Prostaglandin Antagonists
Receptors, Prostaglandin E
Receptors, Prostaglandin E, EP3 Subtype
Sulfonamides