Chemical & Pharmaceutical Bulletin 1999-02-01

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

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

文献索引：Chem. Pharm. Bull. 47(2) , 177-81, (1999)

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摘要

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.).