Here, two series of novel ursolic acid-based 1,2,4-triazolo[1,5-a]pyrimidines derivatives were synthesized and screened for their anti-inflammatory activity by evaluating their inhibition effect of using LPS-induced inflammatory response in RAW 264.7 macrophages in vitro; the effects of different concentrations of the compounds on the secretion of nitric oxide (NO) and inflammatory cytokines including TNF-α and IL-6 were evaluated. Their toxicity was also assessed in vitro. Results showed that the most prominent compound 3 could significantly decrease production of the above inflammatory factors. Docking study was performed for the representative compounds 3, UA, and Celecoxib to explain their interaction with cyclooxygenase-2 (COX-2) receptor active site. In vitro enzyme study implied that compound 3 exerted its anti-inflammatory activity through COX-2 inhibition.

在这里，合成了两个基于熊果酸的新型 1,2,4-三唑并[1,5-a]嘧啶衍生物，并通过评估它们在 RAW 中使用 LPS 诱导的炎症反应的抑制作用来筛选它们的抗炎活性。 264.7 体外巨噬细胞；评估了不同浓度的化合物对一氧化氮（NO）和炎症细胞因子（包括TNF-α和IL-6）分泌的影响。还在体外评估了它们的毒性。结果表明，最显着的化合物3可以显着减少上述炎症因子的产生。对代表性化合物3、UA、塞来昔布进行对接研究解释它们与环氧合酶2（COX-2）受体活性位点的相互作用。体外酶研究表明化合物3通过抑制 COX-2 发挥其抗炎活性。