Structure-activity relationships and in vivo activity of (1H-pyrazol-4-yl)acetamide antagonists of the P2X sub(7) receptor

Structure-activity relationships (SAR) of analogues of lead compound 1 were investigated and compound 16 was selected for further study in animal models of pain. Compound 16 was shown to be a potent antihyperalgesic agent in both the rat acute complete Freund's adjuvant (CFA) model of inflammat...

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Published inBioorganic & medicinal chemistry letters Vol. 20; no. 15; pp. 4653 - 4656
Main Authors Beswick, Paul J, Billinton, Andy, Chambers, Laura J, Dean, David K, Fonfria, Elena, Gleave, Robert J, Medhurst, Stephen J, Michel, Anton D, Moses, Andrew P, Patel, Sadhana, Roman, Shilina A, Roomans, Sue, Senger, Stefan, Stevens, Alexander J, Walter, Daryl S
Format Journal Article
LanguageEnglish
Published 01.08.2010
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Summary:Structure-activity relationships (SAR) of analogues of lead compound 1 were investigated and compound 16 was selected for further study in animal models of pain. Compound 16 was shown to be a potent antihyperalgesic agent in both the rat acute complete Freund's adjuvant (CFA) model of inflammatory pain [Iadarola, M. J.; Douglass, J.; Civelli, O.; Naranjo, J. R. rain Res. 1988, 455, 205] and the knee joint model of chronic inflammatory pain [Wilson, A. W.; Medhurst, S. J.; Dixon, C. I.; Bontoft, N. C.; Winyard, L. A.; Brackenborough, K. T.; de Alba, J.; Clarke, C. J.; Gunthorpe, M. J.; Hicks, G. A.; Bountra, C.; McQueen, D. S.; Chessell, I. P. Eur. J. Pain 2006, 10, 537].
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ISSN:0960-894X
DOI:10.1016/j.bmcl.2010.05.107