Referenced in: none

Automatically associated channels: TRP , TRPV , TRPV1

Title: Tetrahydro-naphthols as orally available TRPV1 inhibitors.

Authors: Klaus Urbahns, Takeshi Yura, Jang B Gupta, Masaomi Tajimi, Hiroshi Fujishima, Tsutomu Masuda, Noriyuki Yamamoto, Yuka Ikegami, Makiko Marumo, Kayo Yasoshima, Nagahiro Yoshida, Toshiya Moriwaki, David Madge, Fiona Chan, Muneto Mogi

Journal, date & volume: Bioorg. Med. Chem. Lett., 2012 May 15 , 22, 3408-11

PubMed link: http://www.ncbi.nlm.nih.gov/pubmed/22525313

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.