Bioorganic and Medicinal Chemistry Letters p. 1750 - 1754 (2007)
Update date:2022-08-03
Topics:
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.
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.
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