Synthesis of Benzimidazole Derivatives as Antiallergic Agents with 5-Lipoxygenase Inhibiting Action

Syntheses were conducted of novel benzimidazole derivatives that suppress histamine release from mast cells, inhibit 5-lipoxygenase, and possess antioxidative action. Among the compounds synthesized, 1-[2-[2-(4-hydroxy-2, 3, 5-trimethylphenoxy)ethoxy]ethyl]-2-(4-methyl-1-homopiperazino)benzimidazole...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 1999/11/15, Vol.47(11), pp.1573-1578
Hauptverfasser:	NAKANO, Hiroyuki, INOUE, Tsutomu, KAWASAKI, Nobuhide, MIYATAKA, Hideki, MATSUMOTO, Hitoshi, TAGUCHI, Takeo, INAGAKI, Naoki, NAGAI, Hiroichi, SATOH, Toshio
Format:	Artikel
Sprache:	eng
Schlagworte:	5-lipoxygenase Animals Anti-Allergic Agents - chemical synthesis Anti-Allergic Agents - chemistry Anti-Allergic Agents - pharmacology antiallergic agent antioxidative action benzimidazole Benzimidazoles - chemical synthesis Benzimidazoles - chemistry Benzimidazoles - pharmacology Biological and medical sciences Guinea Pigs histamine Histamine and antagonists. Allergy Ileum - drug effects Lipid Peroxidation - drug effects Lipoxygenase Inhibitors - chemical synthesis Lipoxygenase Inhibitors - chemistry Lipoxygenase Inhibitors - pharmacology Magnetic Resonance Spectroscopy Male Medical sciences Microsomes, Liver - drug effects Microsomes, Liver - metabolism Molecular Structure Pharmacology. Drug treatments Rats Rats, Wistar Spectrometry, Mass, Fast Atom Bombardment Tumor Cells, Cultured
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Zusammenfassung:	Syntheses were conducted of novel benzimidazole derivatives that suppress histamine release from mast cells, inhibit 5-lipoxygenase, and possess antioxidative action. Among the compounds synthesized, 1-[2-[2-(4-hydroxy-2, 3, 5-trimethylphenoxy)ethoxy]ethyl]-2-(4-methyl-1-homopiperazino)benzimidazole (22) potently suppressed histamine release from rat peritoneal mast cells triggered by the antigen-antibody reaction, inhibited 5-lipoxygenase in rat basophilic leukemia-1 (RBL-1) cells, and prevented the NADPH-dependent lipid peroxidation induced by Fe3+-ADP in rat liver microsomes, in addition to an antagonizing the contraction of guinea pig ileum caused by histamine.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.47.1573