作为具有抗氧化作用的抗过敏剂的三甲基氢醌衍生物的合成。

Synthesis of trimethylhydroquinone derivatives as anti-allergic agents with anti-oxidative actions.

作者信息

Kawasaki N, Miyataka H, Nishiki M, Matsumoto H, Inagaki N, Nagai H, Satoh T

机构信息

Faculty of Pharmaceutical Sciences, Tokushima Bunri University, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1999 Feb;47(2):177-81. doi: 10.1248/cpb.47.177.

DOI:10.1248/cpb.47.177

PMID:10071852

Abstract

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 Fe(3+)-ADP induced NADPH dependent lipid peroxidation (IC50 = 5.3 x 10(-7) M), 5-lipoxygenase ((IC50 = 3.5 x 10(-7) M) and PCA reaction (57% inhibition at 100 mg/kg p.o.).

摘要

合成了一系列新型的三甲基氢醌衍生物，并对其在大鼠肝微粒体中的抗脂质过氧化活性、对大鼠嗜碱性白血病-1（RBL-1）细胞5-脂氧合酶的抑制作用以及在大鼠中48小时同源被动皮肤过敏反应（PCA）活性进行了评估。4-[4-[4-(二苯甲基)-1-哌嗪基]-丁氧基]-2,3,6-三甲基苯酚（9c）表现出抑制Fe(3+)-ADP诱导的NADPH依赖性脂质过氧化的能力（IC50 = 5.3 x 10(-7) M）、5-脂氧合酶（IC50 = 3.5 x 10(-7) M）以及PCA反应（口服100 mg/kg时抑制率为57%）。