Results 261 to 270 of about 44,003 (300)
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Agents and Actions, 1985
Studies on the combined effects of a variety of lipoxygenase inhibitors and cyclo-oxygenase inhibitors revealed strong evidence for the existence of supplementary binding sites on lipoxygenases which modify the reactions of inhibitors with the catalytic site of the enzyme.
J, Baumann, G, Wurm, I, Baumann
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Studies on the combined effects of a variety of lipoxygenase inhibitors and cyclo-oxygenase inhibitors revealed strong evidence for the existence of supplementary binding sites on lipoxygenases which modify the reactions of inhibitors with the catalytic site of the enzyme.
J, Baumann, G, Wurm, I, Baumann
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[Inhibitors of 5-lipoxygenase].
Ceska a Slovenska farmacie : casopis Ceske farmaceuticke spolecnosti a Slovenske farmaceuticke spolecnosti, 2002Leukotrienes 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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5-Lipoxygenase Inhibitors for the Treatment of COPD
Chest, 2002The potential for leukotrienes as mediators to target in the development of novel therapies for diseases such as COPD is underscored by their inflammatory behavior and the capacity of leukotriene receptor antagonists and synthesis inhibitors to reduce inflammatory responses when administered in vivo.
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New Bis-catechols 5-lipoxygenase inhibitors
Bioorganic & Medicinal Chemistry, 2001Three polyhydroxy-2-phenylnaphthalenes (1-3) and the oxy analogue of tetrahydroxypavinan (4) were prepared and evaluated for their antioxidant properties (inhibition of diphenylpycrylhydrazyl radical (DPPH), reduction of iron (III) ion) and inhibition of 5-lipoxygenase (5-LO) activity. Their three-dimensional structures were established on the basis of
Dupont, R. +6 more
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Inhibitors of the 5-Lipoxygenase Pathway in Atherosclerosis
Current Pharmaceutical Design, 2009The inflammatory environment within the atherosclerotic lesion stimulates the 5-lipoxygenase pathway of arachidonic acid metabolism, leading to the biosynthesis of the potent lipid inflammatory mediators leukotrienes. The present review summarizes the components of this pathway; the enzymes 5-lipoxygenase (5-LO, ALOX5) with its activating protein, FLAP
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Eicosatetraenehydroxamates: inhibitors of 5-lipoxygenase
Tetrahedron Letters, 1985Abstract 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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Biochemical Pharmacology, 1988
Soybean lipoxygenase is rapidly inactivated when incubated with arachidonic acid and any of several lipoxygenase inhibitors, including NDGA, the aminopyrazolines BW 755C and BW 540C, and the acetohydroxamic acid derivatives BW A4C and BW A137C. Little or no inactivation was found when the enzyme was incubated with substrate or with inhibitors alone. 15-
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Soybean lipoxygenase is rapidly inactivated when incubated with arachidonic acid and any of several lipoxygenase inhibitors, including NDGA, the aminopyrazolines BW 755C and BW 540C, and the acetohydroxamic acid derivatives BW A4C and BW A137C. Little or no inactivation was found when the enzyme was incubated with substrate or with inhibitors alone. 15-
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Novel bishydroxamic acids as 5-lipoxygenase inhibitors
Bioorganic & Medicinal Chemistry, 1994Two series of novel bishydroxamic acids 2 and 3 (types A and B) were synthesized and tested for inhibition of 5-lipoxygenase from rat basophile leukemia (RBL) cells. Both series were potent inhibitors of the isolated enzyme but only the type B reverse hydroxamic acids possessed significant oral activity. The most potent compound, orally, was 3a, [IC50 =
K A, Ohemeng +6 more
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Photoactivation of an Inhibitor of the 12/15‐Lipoxygenase Pathway
ChemBioChem, 2006AbstractLipoxygenases are lipid‐peroxidizing enzymes that have been implicated in the pathogenesis of inflammatory diseases and lipoxygenase inhibitors may be developed as anti‐inflammatory drugs. Structure comparison with known lipoxygenase inhibitors has suggested that (2Z)‐2‐(3‐benzylidene)‐3‐oxo‐2,3‐dihydrobenzo[b]thiophene‐7‐carboxylic acid methyl
Stephan, Herre +7 more
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Lipoxygenase Inhibitors for Cancer Prevention: Promises and Risks
Current Pharmaceutical Design, 2010It is well established that an increase of n-6 polyunsaturated (i.e. arachidonic and arachidonic-converted linoleic acids) fat dietary intake enhances carcinogenesis and promotes tumorigenesis through oxidative metabolism. The Cyclooxygenase (COX) and Lipoxygenase (LOX) enzymes mediate the oxidative metabolism of n-6 polyunsaturated fatty acids and ...
Cecilia, Menna +3 more
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