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Identification of potent, soluble, and orally active TRPV1 antagonists.
Bioorganic & Medicinal Chemistry Letters 2011 April 16
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.
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