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Review: lipoxygenase inhibitors and the gut

Alimentary Pharmacology & Therapeutics, 1987
SUMMARYLeukotriene synthesis is influenced by several drugs currently in use for the treatment of alimentary disease, including the corticosteroids, sulphasalazine and mesalazine. However, the use of selective lipoxygenase inhibitors in human gastrointestinal disease has not been investigated. The complexity of eicosanoid metabolism, and the incomplete
N P, Kennedy, P W, Keeling
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Designing therapeutically effective 5-lipoxygenase inhibitors

Trends in Pharmacological Sciences, 1992
Metabolism of arachidonic acid by the enzyme 5-lipoxygenase leads to the formation of a group of biologically active lipids known as leukotrienes. Peptidoleukotrienes are powerful bronchoconstrictor agents while leukotriene B4 is a potent chemotactic agent for a variety of leukocytes.
R M, McMillan, E R, Walker
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Therapeutic options for 5-lipoxygenase inhibitors

Pharmacology & Therapeutics, 2006
5-Lipoxygenase (5-LO) catalyzes the conversion of arachidonic acid (AA) into leukotriene (LT) A(4) and 5-hydroperoxyeicosatetraenoic acid. LTA(4) can then be converted into LTB(4) by LTA(4) hydrolase or into LTC(4) by LTC(4) synthase and the LTC(4) synthase isoenzymes MGST2 and MGST3.
Oliver, Werz, Dieter, Steinhilber
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A lipoxygenase inhibitor from Aspergillus niger

Applied Microbiology and Biotechnology, 2002
A lipoxygenase-1 (LOX-1) inhibitor was isolated from the fermented broth of Aspergillus niger CFTRI 1105. It was purified, using column and preparative thin layer chromatography. 1H NMR and GC-MS examination revealed the structure of the inhibitor to be 2-(2'-methyl, 4'-hydroxyphenyl), 2-(4"hydroxyphenyl)-propane with a molecular weight of 242 and the ...
Rao K C, Sekhar   +4 more
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Conversion of cyclooxygenase inhibitors into hydroxythiazole 5-lipoxygenase inhibitors

Bioorganic & Medicinal Chemistry, 1997
Representative examples of NSAID cyclooxygenase inhibitors such as naproxen, ibufenac, ibuprofen, and butibufen have been transformed into 5-lipoxygenase inhibitors by replacement of the carboxylic acid moiety with a 4-hydroxythiazole group.
F A, Kerdesky   +4 more
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Lipoxygenase inhibitor from Lactobacillus casei

Biotechnology Letters, 2002
An inhibitor of plant lipoxygenase from culture filtrates of Lactobacillus casei was purified by column chromatography and shown to be benzoic acid. The isolated benzoic acid had an IC50 of 350 μM against purified soybean lipoxygenase at pH 9. L. casei therefore may have the potential to be used as a preservative against the oxidation of unsaturated ...
K.C. Sekhar Rao   +4 more
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Eicosatetraenehydroxamates: inhibitors of 5-lipoxygenase

Tetrahedron Letters, 1985
Abstract The syntheses of 5-hydroxamyl and 5-hydroxamylmethyl-6,8,11,14,-eicosatetraenoic acids ( 3 and 4 ), which possess potent 5-lipoxygenase inhibitory activity, are described.
F.A.J. Kerdesky   +4 more
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Inhibitors of 15-Lipoxygenase from Orange Peel

Journal of Agricultural and Food Chemistry, 2000
A series of polymethoxylated flavonoids has been isolated from orange peel, and their inhibitory activity toward soybean 15-lipoxygenase was determined. The strongest inhibition was shown by 3,5,6,7,3',4'-hexamethoxyflavone (IC(50) = 49 +/- 5 microM). Sinensetin, nobiletin, tangeretin, tetramethylscutellarein, and 3,5, 6,7,8,3',4'-heptamethoxyflavone ...
K E, Malterud, K M, Rydland
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5-Lipoxygenase inhibitors: a patent evaluation (WO2011161615)

Expert Opinion on Therapeutic Patents, 2012
1,5-Diarylpyrazoles are privileged scaffolds used for the development of COX-2 (cyclooxygenase 2) selective inhibitors (coxibs). Derivatives of 1,5-diarylpyrazoles are currently being used as 5-lipoxygenase (5-LO) inhibitors for the treatment of respiratory diseases, inflammatory and autoimmune disorders.
Estel la, Buscató, Ewgenij, Proschak
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[Inhibitors of 5-lipoxygenase].

Ceska a Slovenska farmacie : casopis Ceske farmaceuticke spolecnosti a Slovenske farmaceuticke spolecnosti, 2002
Leukotrienes are powerful mediators of inflammation processes. Possibilities of their biosynthesis inhibition have been intensively studied during recent two decades aiming to develop new methods of therapy of various inflammatory diseases, particularly asthma. Biosynthesis of all leukotrienes is dependent on the production of the key intermediate LTA4.
M, Gápovský, M, Remko
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