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Synthesis and biological activities of novel antiallergic agents with 5-lipoxygenase inhibiting action.

Abstract：

:Novel benzimidazole derivatives were synthesized and their pharmacological activities were examined. These compounds showed a good suppressive action on histamine release from rat peritoneal mast cells produced by antigen-antibody reaction, an antagonistic action on guinea pig ileum contraction caused by histamine, an inhibitory action on 5-lipoxygenase in rat basophilic leukemia-1 (RBL-1) cells, and a preventive action on NADPH dependent lipid peroxidation induced by Fe3+-ADP in rat liver microsomes. In addition, 1-[2-[2-(4-Hydroxy-2,3,5-trimethylphenoxy)ethoxy]-ethyl]-2-(4-meth yl-1-homopiperazino)-1H-benzimidazole difumarate (BOM1006) exhibited a dose dependent suppressive action on 48 h homologous passive cutaneous anaphylaxis (PCA) reaction in rats orally administered the drug.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Nakano H,Inoue T,Kawasaki N,Miyataka H,Matsumoto H,Taguchi T,Inagaki N,Nagai H,Satoh T

doi

10.1016/s0968-0896(99)00291-6

subject

Has Abstract

pub_date

2000-02-01 00:00:00

pages

373-80

issue

2

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(99)00291-6

journal_volume

8

pub_type

杂志文章

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