Synthesis of benzamide derivatives as TRPV1 antagonists |
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| Authors: | Shishido Yuji Jinno Madoka Ikeda Takafumi Ito Fumitaka Sudo Masaki Makita Naoya Ohta Atsuko Iki-Taki Ayako Ohmi Takashi Kanai Yoshihito Tamura Tetsuya Shimojo Masato |
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| Affiliation: | Pfizer Global Research & Development, Nagoya Laboratories, 5-2 Taketoyo, Aichi 470-2394, Japan. Yuji.Shishido@pfizer.com |
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| 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 IC(50)=23 nM, (+/-)-3: human IC(50)=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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