5-甲氧基色胺类衍生物的合成及抗痒活性评价

以5-甲氧基色胺为基本骨架,与肉桂酸衍生物或苯乙酸衍生物进行酰胺化反应,得到3个新型的5-甲氧基色胺衍生物Ca1、Ca2、Ca3。化合物结构通过IR、1H NMR和元素分析进行确证,并且测试了目标化合物对瘙痒模型小鼠的抗痒活性。抗痒活性测试结果表明,化合物Ca3具有较强的抗痒活性,有望成为新型的抗痒药物。

Synthesis and Anti- itch Activity Evaluation of 5 - Methoxytryptamine Derivatives

Three 5 -methoxytryptamine derivatives（ Cal, Ca2, and Ca3）were synthesized. They were prepared of 5 -me- thoxytryptamine as the basic skeleton by amidation with phenylacrylic acid or phenylacetic acid derivatives. The structures of compounds were confirmed by IR, 1H NMR spectra and elemental analysis. The anti- itch activity of the target compounds was tested. Results of anti - itch activity evaluation showed that compound Ca3 had high anti - itch activity and it expected to be- come a novel anti -itch drug.