Literature DB >> 12182865

Structure-activity relationship of biaryl acylsulfonamide analogues on the human EP(3) prostanoid receptor.

M Gallant1, M C Carrière, A Chateauneuf, D Denis, Y Gareau, C Godbout, G Greig, H Juteau, N Lachance, P Lacombe, S Lamontagne, K M Metters, C Rochette, R Ruel, D Slipetz, N Sawyer, N Tremblay, M Labelle.   

Abstract

Potent and selective ligands for the human EP3 prostanoid receptor are described. Biaryl compounds bearing a tethered ortho substituted acidic moiety were identified as potent EP3 antagonists based on the SAR described herein. The binding affinity of key compounds on all eight human prostanoid receptors is reported.

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Year:  2002        PMID: 12182865     DOI: 10.1016/s0960-894x(02)00518-8

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  6 in total

1.  Roles of affinity and lipophilicity in the slow kinetics of prostanoid receptor antagonists on isolated smooth muscle preparations.

Authors:  R L Jones; D F Woodward; J W Wang; R L Clark
Journal:  Br J Pharmacol       Date:  2011-02       Impact factor: 8.739

Review 2.  Role of biotransformation studies in minimizing metabolism-related liabilities in drug discovery.

Authors:  Yue-Zhong Shu; Benjamin M Johnson; Tian J Yang
Journal:  AAPS J       Date:  2008-03-13       Impact factor: 4.009

3.  Novel 3-Oxazolidinedione-6-aryl-pyridinones as Potent, Selective, and Orally Active EP3 Receptor Antagonists.

Authors:  Jian Jin; Angel Morales-Ramos; Patrick Eidam; John Mecom; Yue Li; Carl Brooks; Mark Hilfiker; David Zhang; Ning Wang; Dongchuan Shi; Pei-San Tseng; Karen Wheless; Brian Budzik; Karen Evans; Jon-Paul Jaworski; Jack Jugus; Lisa Leon; Charlene Wu; Mark Pullen; Bhumika Karamshi; Parvathi Rao; Emma Ward; Nicholas Laping; Christopher Evans; Colin Leach; Dennis Holt; Xin Su; Dwight Morrow; Harvey Fries; Kevin Thorneloe; Richard Edwards
Journal:  ACS Med Chem Lett       Date:  2010-05-14       Impact factor: 4.345

4.  Interaction of prostanoid EP₃ and TP receptors in guinea-pig isolated aorta: contractile self-synergism of 11-deoxy-16,16-dimethyl PGE₂.

Authors:  R L Jones; D F Woodward
Journal:  Br J Pharmacol       Date:  2011-01       Impact factor: 8.739

Review 5.  Prostanoid receptor antagonists: development strategies and therapeutic applications.

Authors:  R L Jones; M A Giembycz; D F Woodward
Journal:  Br J Pharmacol       Date:  2009-07-15       Impact factor: 8.739

6.  Prostaglandin E2 mediates cough via the EP3 receptor: implications for future disease therapy.

Authors:  Sarah A Maher; Mark A Birrell; Maria G Belvisi
Journal:  Am J Respir Crit Care Med       Date:  2009-09-03       Impact factor: 21.405

  6 in total

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