3-Ylidenephthalides as a new class of transient receptor potential channel TRPA1 and TRPM8 modulators
作者:Giorgio Ortar、Aniello Schiano Moriello、Enrico Morera、Marianna Nalli、Vincenzo Di Marzo、Luciano De Petrocellis
DOI:10.1016/j.bmcl.2013.08.039
日期:2013.10
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.