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

…, E Morera, M Nalli, V Di Marzo, L De Petrocellis

Index: Ortar, Giorgio; Schiano Moriello, Aniello; Morera, Enrico; Nalli, Marianna; Di Marzo, Vincenzo; De Petrocellis, Luciano Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 20 p. 5614 - 5618

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Citation Number: 14

Abstract

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 EC 50 and/or IC 50 values distinctly lower than those of the ...

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