Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, piazzale Aldo Moro 5, 00185 Roma, Italy.
Bioorg Med Chem Lett. 2013 Oct 15;23(20):5614-8. doi: 10.1016/j.bmcl.2013.08.039. Epub 2013 Aug 14.
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.
最近发现天然存在的 3-亚甲基-4,5-二氢苯酞藁本内酯及其氧化产物脱水藁本内酯是新型的 TRPA1 调节剂，因此我们合成了一系列十七个 3-亚苯基苯酞，并对 TRPA1 和 TRPM8 通道进行了测试。这些化合物中的大多数对两种通道类型均表现出较强的调制作用，其 EC50 和/或 IC50 值明显低于对照化合物。
