335416-47-2Relevant academic research and scientific papers
Identification of novel glycine sulfonamide antagonists for the EP1 receptor
McKeown, Stephen C.,Hall, Adrian,Blunt, Richard,Brown, Susan H.,Chessell, Iain P.,Chowdhury, Anita,Giblin, Gerard M.P.,Healy, Mark P.,Johnson, Matthew R.,Lorthioir, Olivier,Michel, Anton D.,Naylor, Alan,Lewell, Xiao,Roman, Shilina,Watson, Stephen P.,Winchester, Wendy J.,Wilson, Richard J.
, p. 1750 - 1754 (2007/10/03)
A high-throughput screen targeting the EP1 receptor identified non-acidic glycine sulfonamide derivative 2a with a pKi of 6.2. Analogue synthesis allowed a thorough investigation of the structure-activity relationship (SAR) and led to a 100-fold increase in recombinant potency.
Identification and optimization of novel 1,3,4-oxadiazole EP1 receptor antagonists
Hall, Adrian,Brown, Susan H.,Chowdhury, Anita,Giblin, Gerard M.P.,Gibson, Mairi,Healy, Mark P.,Livermore, David G.,McArthur Wilson, Richard J.,Naylor, Alan,Rawlings, D. Anthony,Roman, Shilina,Ward, Emma,Willay, Caroline
, p. 4450 - 4455 (2008/02/10)
A novel series of oxadiazole EP1 receptor antagonists was identified by replacing the amide of a known glycine sulfonamide derivative with a 1,3,4-oxadiazole. Optimization of the substitution patterns on the three aromatic rings led to the iden
