A novel series of potent and selective EP(4) receptor ligands: facile modulation of agonism and antagonism.
Basic Information
ID: ALA1641558
Journal: Bioorg Med Chem Lett
Title: A novel series of potent and selective EP(4) receptor ligands: facile modulation of agonism and antagonism.
Authors: Boyd MJ, Berthelette C, Chiasson JF, Clark P, Colucci J, Denis D, Han Y, Lévesque JF, Mathieu MC, Stocco R, Therien A, Rowland S, Wrona M, Xu D.
Abstract: A novel series of EP(4) ligands, based on a benzyl indoline scaffold, has been discovered. It was found that agonism and antagonism in this series can be easily modulated by minor modifications on the benzyl group. The pharmacokinetic, metabolic and pharmacological profiles of these compounds was explored. It was found that these compounds show good pharmacokinetics in rat and are efficacious in pre-clinical models of pain and inflammation.
CiteXplore: 21126875
DOI: 10.1016/j.bmcl.2010.10.106
Patent ID: ┄