Structure-activity studies of a novel series of isoxazole-3-carboxamide derivatives as TRPV1 antagonists.

Ronald Palin, Lynn Abernethy, Nasrin Ansari, Kenneth Cameron, Tom Clarkson, Maureen Dempster, David Dunn, Anna-Marie Easson, Darren Edwards, John Maclean, Katy Everett, Helen Feilden, Koc-Kan Ho, Steve Kultgen, Peter Littlewood, Duncan McArthur, Deborah McGregor, Hazel McLuskey, Irina Neagu, Stuart Neale, Lesley-Anne Nisbet, Michael Ohlmeyer, Quynhchi Pham, Paul Ratcliffe, Yajing Rong, Andrew Roughton, Melanie Sammons, Robert Swanson, Heather Tracey, Glenn Walker

Bioorganic & Medicinal Chemistry Letters 2011 Februrary 2

Optimisation of a screening hit incorporating both TRPV1 activity and solubility was conducted. Substitution of the isoxazole-3-carboxamide with the bespoke 1S, 3R-3-aminocyclohexanol motif afforded the requisite balance of potency and solubility. Compounds 32 and 40 were found to have antihyperalgesic effects in the rat CFA Hg assay and induce a mechanism based hyperthermia.

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