新型NK1受体拮抗剂的合成及生物活性研究
Synthesis and bioactivity of novel NK1 receptor antagonists
作者：和龙;向洪刚;刘新琦;温晓燕;王玲;欧阳亮;何俊;
Author：
收稿日期： 年卷（期）页码：2019,34(04):-332-336
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：N-甲基-N-(4-(2-苯甲基)-6-(4-甲基-1-哌嗪基)-3-吡啶基)苯甲酰胺衍生物;合成;生物活性;NK1受体;钙流实验;HEK293/NK1R细胞株;拮抗活性
Key words：
基金项目：四川省应用基础研究项目(2019YJ0108);;
川大-泸州战略合作基金(2015CDLZ-S10)
中文摘要
目的制备一类新型N-甲基-N-(4-(2-苯甲基)-6-(4-甲基-1-哌嗪基)-3-吡啶基)苯甲酰胺衍生物,并评价其对NK1受体的体外拮抗活性。方法以6-(4-甲基-1-哌嗪基)-4-(2-甲基苯基)烟酰胺为起始原料,经过霍夫曼降解、酰胺还原和N-酰化等化学反应得到目标化合物;采用钙流实验,在HEK293/NK1R细胞株上进行体外对NK1受体拮抗活性的测定。结果制备了13个新型化合物(Ⅰ_1～Ⅰ_(13)),并经~1HNMR确证结构。化合物Ⅰ_(12)对HEK293/NK1R细胞有较好的NK1受体拮抗活性。结论化合物Ⅰ_(12)作为一类新型NK1受体拮抗剂,具有深入研究的价值。
参考文献
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