Article ID Journal Published Year Pages File Type
1369772 Bioorganic & Medicinal Chemistry Letters 2012 4 Pages PDF
Abstract

Starting from a naphthol-based lead series with low oral bioavailability, we have identified potent TRPV1 antagonists with oral bioavailability in rats. These compounds emerged from SAR studies aimed at replacing the lead’s phenol structure whilst maintaining potency. Compound rac-6a is an orally available TRPV1 antagonist with single-digit nanomolar activity. The enantiomers show a low eudismic ratio at the receptor level.

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Related Topics
Physical Sciences and Engineering Chemistry Organic Chemistry
Authors
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