Wang Zheng, Bae Eun Ju, Han Young Taek
College of Pharmacy, Woosuk University, Wanju, 55338, Korea.
College of Pharmacy, Dankook University, Cheonan, 31116, Korea.
Arch Pharm Res. 2017 Jun;40(6):695-703. doi: 10.1007/s12272-017-0910-5. Epub 2017 Apr 10.
A novel series of dihydropyranoaurone derivatives were synthesized and evaluated as potential anti-inflammatory agents. Late-stage derivatization by versatile piperazine-catalyzed aldol reaction between dihydropyanobenzofuran intermediate 2 and diverse aldehydes readily afforded the novel dihydropyranoaurone analogs. Evaluation of the synthesized dihydropyranoaurone derivatives and related compounds regarding their inhibiting inducible nitric oxide synthase and nitrite production of lipopolysaccaride-stimulated RAW 264.7 cells provided insight into the structure-activity relationship of aurone derivatives.
合成了一系列新型二氢吡喃奥酮衍生物，并将其作为潜在的抗炎剂进行评估。通过二氢吡喃苯并呋喃中间体2与各种醛之间通用的哌嗪催化羟醛反应进行后期衍生化，很容易得到新型二氢吡喃奥酮类似物。对合成的二氢吡喃奥酮衍生物及相关化合物抑制脂多糖刺激的RAW 264.7细胞中诱导型一氧化氮合酶和亚硝酸盐产生的情况进行评估，为奥酮衍生物的构效关系提供了深入了解。
