摘要
以NLRP3炎症小体为靶点,设计并合成了一系列α,β-不饱和酮类化合物,并测定了其体外抗炎活性。发现数个化合物有强的抑制IL-1β释放的抗炎活性,其中A21表现出最强的抗炎活性,并呈剂量依赖关系,其IC_(50)为0.95μM。论文中还总结了该类化合物初步的构效关系。
A series of α,β-unsaturated ketone derivatives were synthesized, and their anti-inflammatory activity toward NLRP3 inflammasome was evaluated in vitro. Several compounds were identified as anti-inflammatory agents, among which compound A21 exhibited potent anti-inflammatory activity in a dose-dependent manner with an IC50)of 0.95 μM. Moreover, a preliminary structure-activity relationship was also summarized.
作者
孔秋云
杭楠
张超
李树春
李中军
孙洋
孟祥豹
Qiuyun Kong;Nan Hang;Chao Zhang;Shuchun Li;Zhongjun Li;Yang Sun;Xiangbao Meng(State Key Laboratory of Natural and Biomimetic Drugs," Department of Chemical Biology, School of Pharmaceutical Sciences Peking University, Beijing 100191, China;State Key Laboratory of Pharmaceutical Biotechnology, School of Life Sciences, Nanjing University, Nanjing 210023, China)
基金
The National Natural Science Foundation of China(Grant No.81573272)