以水杨酸为起始原料,经Fridel—Crafts酰基化反应、微波促进的Perkin反应和两步亲核取代反应,合成了具有氨基烷氧侧链的3,4-二苯基香豆素衍生物ladle.初步生物活性测试表明,化合物ladle能显著促进自然杀伤细胞杀伤活性,具有较强的免疫调节活性.
A series of novel 3,4-biphenyl coumarin derivatives containing an amino side chain ladle were synthesized using salicylic acid as starting material via Fridel-Crafts acylation, then the microwave-assisted Perkin reaction and double SN2 sub- stitution reactions. The preliminary biological evaluation showed that compounds ladle had significant promoting effects on the killing activity of natural killer cell, and hold potential as immunomodulating agents.