Synthesis of benzamide derivatives as TRPV1 antagonists
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Add time:08/25/2019 Source:sciencedirect.com
From hit compounds identified by high throughput screening (HTS), we have found compound 1 as a lead TRPV1 antagonist and confirmed its potential as a treatment for pain. Compound 1 has led to potent TRPV1 antagonistic benzamide derivatives ((±)-2: human IC50 = 23 nM, (±)-3: human IC50 = 14 nM in the capsaicin-induced calcium influx assay) containing indole and naphthyl moieties, obtained by elaboration of the tryptamine scaffold or via bioisosteric replacements.
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