Modulation of thermo-transient receptor potential (thermo-TRP) channels by thymol-based compounds

Bioorg Med Chem Lett. 2012 May 15;22(10):3535-9. doi: 10.1016/j.bmcl.2012.03.055. Epub 2012 Mar 20.

Abstract

A series of thirty-three thymol, p-cymene-3-carboxylic acid, and 3-amino-p-cymene derivatives was synthesized and tested on TRPA1, TRPM8, and TRPV3 channels. Most of them acted as strong modulators of TRPA1, TRPM8, and TRPV3 channels with EC(50) and/or IC(50) values distinctly lower than those of thymol and related monoterpenoids. Some of the compounds examined, that is, 3c, 4e, f, 6b, and 8b exhibited an appreciable subtype-selectivity.

MeSH terms

  • Animals
  • Cell Line
  • Humans
  • Rats
  • Thymol / chemistry
  • Thymol / pharmacology*
  • Transient Receptor Potential Channels / drug effects*

Substances

  • Transient Receptor Potential Channels
  • Thymol