3-Ylidenephthalides as a new class of transient receptor potential channel TRPA1 and TRPM8 modulators

  • Bioorg Med Chem Lett. 2013 Oct 15;23(20):5614-8. doi: 10.1016/j.bmcl.2013.08.039.
Giorgio Ortar  1 ,  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, piazzale Aldo Moro 5, 00185 Roma, Italy. Electronic address: [email protected].
PMID: 23993334 DOI: 10.1016/j.bmcl.2013.08.039
Abstract

Following the recent identification of the naturally occurring 3-ylidene-4,5-dihydrophthalide ligustilide and its oxidation product dehydroligustilide as novel TRPA1 modulators, a series of seventeen 3-ylidenephthalides was synthesized and tested on TRPA1 and TRPM8 channels. Most of these compounds acted as strong modulators of the two channel types with EC50 and/or IC50 values distinctly lower than those of the reference compounds.

Keywords
3-Ylidenephthalides; TRPA1; TRPM8; Transient receptor potential channels.