Identification of novel glycine sulfonamide antagonists for the EP1 receptor.

ID: ALA1139103

Journal: Bioorg Med Chem Lett

Title: Identification of novel glycine sulfonamide antagonists for the EP1 receptor.

Authors: McKeown SC, Hall A, Blunt R, Brown SH, Chessell IP, Chowdhury A, Giblin GM, Healy MP, Johnson MR, Lorthioir O, Michel AD, Naylor A, Lewell X, Roman S, Watson SP, Winchester WJ, Wilson RJ.

Abstract: A high-throughput screen targeting the EP(1) receptor identified non-acidic glycine sulfonamide derivative 2a with a pK(i) 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.

CiteXplore: 17236765

DOI: 10.1016/j.bmcl.2006.12.060

Patent ID: ┄