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Literature DB >> 10722160

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

H Nakano¹, T Inoue, N Kawasaki, H Miyataka, H Matsumoto, T Taguchi, N Inagaki, H Nagai, T Satoh.

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.

Entities: Chemical Disease Gene Species

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Year: 2000 PMID： 10722160 DOI： 10.1016/s0968-0896(99)00291-6

Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641

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Cited

21 in total

1. Synthesis and structure-activity relationship studies of 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase.

Authors: Diane K Luci; J Brian Jameson; Adam Yasgar; Giovanni Diaz; Netra Joshi; Auric Kantz; Kate Markham; Steve Perry; Norine Kuhn; Jennifer Yeung; Edward H Kerns; Lena Schultz; Michael Holinstat; Jerry L Nadler; David A Taylor-Fishwick; Ajit Jadhav; Anton Simeonov; Theodore R Holman; David J Maloney
Journal: J Med Chem Date: 2014-01-06 Impact factor: 7.446

2. Discovery of potent and selective inhibitors of human platelet-type 12- lipoxygenase.

Authors: Victor Kenyon; Ganesha Rai; Ajit Jadhav; Lena Schultz; Michelle Armstrong; J Brian Jameson; Steven Perry; Netra Joshi; James M Bougie; William Leister; David A Taylor-Fishwick; Jerry L Nadler; Michael Holinstat; Anton Simeonov; David J Maloney; Theodore R Holman
Journal: J Med Chem Date: 2011-07-08 Impact factor: 7.446

3. Discovery of potent and selective inhibitors of human reticulocyte 15-lipoxygenase-1.

Authors: Ganesha Rai; Victor Kenyon; Ajit Jadhav; Lena Schultz; Michelle Armstrong; J Brian Jameson; Eric Hoobler; William Leister; Anton Simeonov; Theodore R Holman; David J Maloney
Journal: J Med Chem Date: 2010-10-28 Impact factor: 7.446

4. Investigating inner-sphere reorganization via secondary kinetic isotope effects in the C-H cleavage reaction catalyzed by soybean lipoxygenase: tunneling in the substrate backbone as well as the transferred hydrogen.

Authors: Matthew P Meyer; Judith P Klinman
Journal: J Am Chem Soc Date: 2010-12-30 Impact factor: 15.419

5. Substrate specificity changes for human reticulocyte and epithelial 15-lipoxygenases reveal allosteric product regulation.

Authors: Aaron T Wecksler; Victor Kenyon; Joshua D Deschamps; Theodore R Holman
Journal: Biochemistry Date: 2008-06-21 Impact factor: 3.162

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

1. Synthesis and structure-activity relationship studies of 4-((2-hydroxy-3-methoxybenzyl)amino)benzenesulfonamide derivatives as potent and selective inhibitors of 12-lipoxygenase.

2. Discovery of potent and selective inhibitors of human platelet-type 12- lipoxygenase.

3. Discovery of potent and selective inhibitors of human reticulocyte 15-lipoxygenase-1.

4. Investigating inner-sphere reorganization via secondary kinetic isotope effects in the C-H cleavage reaction catalyzed by soybean lipoxygenase: tunneling in the substrate backbone as well as the transferred hydrogen.

5. Substrate specificity changes for human reticulocyte and epithelial 15-lipoxygenases reveal allosteric product regulation.

6. Investigations of human platelet-type 12-lipoxygenase: role of lipoxygenase products in platelet activation.

7. Kinetic and structural investigations of the allosteric site in human epithelial 15-lipoxygenase-2.

8. Pseudoperoxidase investigations of hydroperoxides and inhibitors with human lipoxygenases.

9. Synthesis of linoleic acids combinatorially-labeled at the vinylic positions as substrates for lipoxygenases.

10. Mechanistic investigations of human reticulocyte 15- and platelet 12-lipoxygenases with arachidonic acid.