Ronnie Palin - Academia.edu (original) (raw)

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Papers by Ronnie Palin

Research paper thumbnail of Discovery of potent, soluble and orally active TRPV1 antagonists. Structure–activity relationships of a series of isoxazoles

Bioorganic & Medicinal Chemistry Letters, 2011

Systematic optimisation of a poorly soluble lead series of isoxazole-3-carboxamides was conducted... more Systematic optimisation of a poorly soluble lead series of isoxazole-3-carboxamides was conducted. Substitution of the 4-position with specific polar functionality afforded the requisite balance of potency, solubility and physicochemical properties. Compound 21a was found to be efficacious in the rat Capsaicin Hargreaves assay following oral administration.

Research paper thumbnail of Identification of potent, soluble, and orally active TRPV1 antagonists

Bioorganic & Medicinal Chemistry Letters, 2011

Optimization of a water soluble, moderately potent lead series of isoxazole-3-carboxamides was co... more 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.

Research paper thumbnail of Discovery of potent, soluble and orally active TRPV1 antagonists. Structure–activity relationships of a series of isoxazoles

Bioorganic & Medicinal Chemistry Letters, 2011

Systematic optimisation of a poorly soluble lead series of isoxazole-3-carboxamides was conducted... more Systematic optimisation of a poorly soluble lead series of isoxazole-3-carboxamides was conducted. Substitution of the 4-position with specific polar functionality afforded the requisite balance of potency, solubility and physicochemical properties. Compound 21a was found to be efficacious in the rat Capsaicin Hargreaves assay following oral administration.

Research paper thumbnail of Identification of potent, soluble, and orally active TRPV1 antagonists

Bioorganic & Medicinal Chemistry Letters, 2011

Optimization of a water soluble, moderately potent lead series of isoxazole-3-carboxamides was co... more 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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