《Design and synthesis of 7-O-1,2,3-triazole hesperetin derivatives to relieve inflammation of acute liver injury in mice》 was written by Zheng, Yan; Zhang, Yi-long; Li, Zeng; Shi, Wen; Ji, Ya-ru; Guo, Ya-Hui; Huang, Cheng; Sun, Guo-ping; Li, Jun. Name: (Bromomethyl)cyclopropaneThis research focused ontriazole hesperetin derivative preparation treatment inflammation acute liver injury; Anti-inflammatory activity introduction; Hesperetin; Structure-activity relationships; Synthesis; Triazole. The article conveys some information:
Based on the previous research results of our research group, to further improve the anti-inflammatory activity of hesperetin, we substituted triazole at the 7-OH branch of hesperetin. We also evaluated the anti-inflammatory activity of 39 new hesperetin derivatives All compounds showed inhibitory effects on nitric oxide (NO) and inflammatory factors in lipopolysaccharide-induced RAW264.7 cells. Compound I, 4-hydroxyimino-7-O-((1-propyl-1H-1,2,3-triazol-4-yl)methyl)hesperetin showed a strong inhibitory effect on NO (half maximal inhibitory concentration = 2.34 ± 0.7μM) and tumor necrosis factor-α, interleukin (IL)-1β, and (IL-6). Structure-activity relationships indicate that 7-O-triazole is buried in a medium-sized hydrophobic cavity that binds to the receptor. Compound 4-hydroxyimino-7-O-((1-propyl-1H-1,2,3-triazol-4-yl)methyl)hesperetin can also reduce the reactive oxygen species production and significantly inhibit the expression of inducible NO synthase and cyclooxygenase-2 through the nuclear factor-κB signaling pathway. In vivo results indicate that compound I can reduce liver inflammation in mice with acute liver injury (ALI) induced by CCI4, and may be a candidate drug for treating inflammation associated with ALI. In the experimental materials used by the author, we found (Bromomethyl)cyclopropane(cas: 7051-34-5Name: (Bromomethyl)cyclopropane)
(Bromomethyl)cyclopropane(cas: 7051-34-5) is used as a synthetic building block for the introduction of the cyclopropylmethyl group. It was also used in the synthesis of 1,4-dienes via iron-catalyzed cross-coupling with alkenyl Grignard reagents.Name: (Bromomethyl)cyclopropane
Referemce:
Bromide – Wikipedia,
bromide – Wiktionary