Bioorganic & Medicinal Chemistry 2000-02-01

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

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

Index: Bioorg. Med. Chem. 8(2) , 373-80, (2000)

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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.