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

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

Affiliation

  • 1 Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, piazzale Aldo Moro 5, 00185 Roma, Italy. Electronic address: giorgio.ortar@uniroma1.it.
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.

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