| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1377346 | Bioorganic & Medicinal Chemistry Letters | 2008 | 7 Pages |
Abstract
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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Related Topics
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Organic Chemistry
Authors
Yuji Shishido, Madoka Jinno, Takafumi Ikeda, Fumitaka Ito, Masaki Sudo, Naoya Makita, Atsuko Ohta, Ayako Iki-Taki, Takashi Ohmi, Yoshihito Kanai, Tetsuya Tamura, Masato Shimojo,