Portal de Periódicos da CAPES

Identification of potent, soluble, and orally active TRPV1 antagonists

2011; Elsevier BV; Volume: 21; Issue: 8 Linguagem: Inglês

10.1016/j.bmcl.2011.01.112

1464-3405

Paul Ratcliffe, John Maclean, Lynn Abernethy, Tom Clarkson, Maureen Dempster, Anna-Marie Easson, Darren Edwards, Katy L. Everett, Helen Feilden, Peter Littlewood, Duncan McArthur, Deborah McGregor, Hazel McLuskey, Olaf Nimz, Lesley-Anne Nisbet, Ronnie Palin, Heather Tracey, Glenn Walker,

Bioactive Compounds and Antitumor Agents

Optimization of a water soluble, moderately potent lead series of isoxazole-3-carboxamides was conducted, affording a compound with the requisite balance of potency, solubility and physicochemical properties for in vivo use. Compound 8e was demonstrated to be efficacious in a rat model of inflammatory pain, following oral administration.