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

Authors
Juteau, HN Gareau, Y Labelle, M Sturino, CF Sawyer, N Tremblay, N Lamontagne, S Carriere, MC Denis, D Metters, KM
Citation
Hn. Juteau et al., Structure-activity relationship of cinnamic acylsulfonamide analogues on the human EP3 prostanoid receptor, BIO MED CH, 9(8), 2001, pp. 1977-1984
Citations number
23
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY
ISSN journal
09680896 → ACNP
Volume
9
Issue
8
Year of publication
2001
Pages
1977 - 1984
Database
ISI
SICI code
0968-0896(200108)9:8<1977:SROCAA>2.0.ZU;2-4
Abstract
Potent and selective antagonists of the human EP3 receptor have been identi fied. The structure-activity relationship of the chemical series was conduc ted and we found several analogues displaying sub-nanomolar K-i values at t he 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. (C) 2001 Elsevier Science Ltd. All rights reserved.