Synthesis and evaluation of ursolic acid-based 1,2,4-triazolo[1,5-a]pyrimidines derivatives as anti-inflammatory agents |
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Authors: | Zhang Tian-Yi Li Chun-Shi Li Ping Bai Xue-Qian Guo Shu-Ying Jin Ying Piao Sheng-Jun |
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Institution: | 1.Jilin Medical University, Jilin, 132013, Jilin Province, People’s Republic of China ;2.The Third People’s Hospital of Dalian, Dalian, 116000, Liaoning Province, People’s Republic of China ;3.Department of General Surgery, Affiliated Hospital of Yanbian University, Yanji, 133000, Jilin Province, People’s Republic of China ; |
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Abstract: | Here, two series of novel ursolic acid-based 1,2,4-triazolo1,5-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. |
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