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Non-acidic pyrazole EP1 receptor antagonists with in vivo analgesic efficacy

Authors :
Hall, Adrian
Billinton, Andy
Brown, Susan H.
Clayton, Nicholas M.
Chowdhury, Anita
Giblin, Gerard M.P.
Goldsmith, Paul
Hayhow, Thomas G.
Hurst, David N.
Kilford, Ian R.
Naylor, Alan
Passingham, Barry
Winyard, Lisa
Source :
Bioorganic & Medicinal Chemistry Letters. Jun2008, Vol. 18 Issue 11, p3392-3399. 8p.
Publication Year :
2008

Abstract

Abstract: Replacement of the carboxylic acid group in a series of previously described methylene-linked pyrazole EP1 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. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
0960894X
Volume :
18
Issue :
11
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
32494106
Full Text :
https://doi.org/10.1016/j.bmcl.2008.04.018