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-ylide-nephthalides 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. (C) 2013 Elsevier Ltd. All rights reserved.
3-Ylidenephthalides as a new class of transient receptor potential channel TRPA1 and TRPM8 modulators / Ortar, Giorgio; Aniello Schiano, Moriello; Morera, Enrico; Nalli, Marianna; Vincenzo Di, Marzo; Luciano De, Petrocellis. - In: BIOORGANIC & MEDICINAL CHEMISTRY LETTERS. - ISSN 0960-894X. - STAMPA. - 23:20(2013), pp. 5614-5618. [10.1016/j.bmcl.2013.08.039]