Chemical and Pharmaceutical Bulletin p. 1573 - 1578 (1999)
Update date:2022-08-03
Topics:
Nakano, Hiroyuki
Inoue, Tsutomu
Kawasaki, Nobuhide
Miyataka, Hideki
Matsumoto, Hitoshi
Taguchi, Takeo
Inagaki, Naoki
Nagai, Hiroichi
Satoh, Toshio
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.
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Doi:10.3987/COM-99-8716
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