Non-acidic pyrazole EP(1) receptor antagonists with in vivo analgesic efficacy

ArticleinBioorganic & medicinal chemistry letters 18(11):3392-9 · July 2008with17 Reads
Impact Factor: 2.42 · DOI: 10.1016/j.bmcl.2008.04.018 · Source: PubMed


    Replacement of the carboxylic acid group in a series of previously described methylene-linked pyrazole EP(1) receptor antagonists led to the discovery of amide, reversed amide and carbamate derivatives. Two compounds, 10a and 10b, were identified as brain penetrant compounds and both demonstrated efficacy in the CFA model of inflammatory pain.