Discovery Of Potent, Soluble And Orally Active Trpv1 Antagonists. Structure-Activity Relationships Of A Series Of Isoxazoles
Bioorganic & medicinal chemistry letters(2011)
摘要
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. (C) 2011 Elsevier Ltd. All rights reserved.
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关键词
TRPV1 antagonist,Antihyperalgesia,Isoxazoles
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