作用于炎症小体的α,β-不饱和酮类化合物的合成及活性评价（英文）

Synthesis and biological evaluation of α,β-unsaturated carbonyl compounds targeting the NLRP3 inflammasome

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.