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Tetrahydro-naphthols as orally available TRPV1 inhibitors |
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| Authors: | Urbahns Klaus Yura Takeshi Gupta Jang B Tajimi Masaomi Fujishima Hiroshi Masuda Tsutomu Yamamoto Noriyuki Ikegami Yuka Marumo Makiko Yasoshima Kayo Yoshida Nagahiro Moriwaki Toshiya Madge David Chan Fiona Mogi Muneto |
| Institution: | Research Center Kyoto, Bayer Yakuhin, Ltd, Kizu, Soraku, Kyoto, Japan. Klaus.Urbahns@merckgroup.com |
| 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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