Affordable Access

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

Authors
  • Nakano, H
  • Inoue, T
  • Kawasaki, N
  • Miyataka, H
  • Matsumoto, H
  • Taguchi, T
  • Inagaki, N
  • Nagai, H
  • Satoh, T
Type
Published Article
Journal
Bioorganic & Medicinal Chemistry
Publisher
Elsevier
Publication Date
Feb 01, 2000
Volume
8
Issue
2
Pages
373–380
Identifiers
PMID: 10722160
Source
Medline
License
Unknown

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.

Report this publication

Statistics

Seen <100 times