Synthesis of Trimethylhydroquinone Derivatives as Anti-allergic Agents with Anti-oxidative Actions.
作者:Nobuhide KAWASAKI、Hideki MIYATAKA、Mayumi NISHIKI、Hitoshi MATSUMOTO、Naoki INAGAKI、Hiroichi NAGAI、Toshio SATOH
DOI:10.1248/cpb.47.177
日期:——
A novel series of trimethylhydroquinone derivatives was synthesized and evaluated for their anti-lipid peroxidation activity in rat liver microsomes, inhibition of rat basophilic leukemia-1 (RBL-1) cell 5-lipoxygenase and 48 h homologous passive cutaneous anaphylaxis (PCA) activity in rats. 4-[4-[4-(Diphenylmethyl)-1-piperazinyl]-butoxy]-2,3,6-trimethyl phenol (9c) exhibited the ability to inhibit
合成了一系列新的三甲基对苯二酚衍生物,并评价了它们在大鼠肝微粒体中的抗脂质过氧化活性,抑制大鼠嗜碱性白血病1(RBL-1)细胞5-脂氧合酶和48h同源被动皮肤过敏(PCA)活性。大鼠。4- [4- [4-(二苯甲基)-1-哌嗪基]-丁氧基] -2,3,6-三甲基苯酚(9c)具有抑制Fe(3 +)-ADP诱导的NADPH依赖性脂质过氧化的能力(IC50 = 5.3×10(-7)M),5-脂氧合酶((IC 50 = 3.5×10(-7)M)和PCA反应(100mg / kg po时抑制57%)。