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.
Giorgio Ortar  1 ,  Ludovica Morera ,  Aniello Schiano Moriello ,  Enrico Morera ,  Marianna Nalli ,  Vincenzo Di Marzo ,  Luciano De Petrocellis
Affiliations
  • 1. Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Roma, Italy. [email protected]
PMID: 22503249 DOI: 10.1016/j.bmcl.2012.03.055
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.