Results 261 to 270 of about 46,425 (297)

Episulfide inhibitors of lipoxygenase

Bioorganic & Medicinal Chemistry Letters, 1992
Abstract A set of epoxide and episulfide substrate mimics were synthesized as inhibitors of soybean lipoxygenase. Enzyme inhibition was observed exclusively with the 12,13-episulfides (1a and 4a), with a high degree of regio- and chemoselectivity. Inhibition by 1a was shown to occur with reduction of the enzyme active site iron from the catalytically
Stephen W. Wright, Mark J. Nelson
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Hydroxamic acid inhibitors of 5-lipoxygenase

Journal of Medicinal Chemistry, 1987
The hydroxamic acid functionality can be incorporated in a variety of simple molecules to produce potent inhibitors of 5-lipoxygenase. As an example of this, the structure-activity relationships in a series of omega-phenylalkyl and omega-naphthylalkyl hydroxamic acids are presented. Among the features described are the influence of hydrophobicity, aryl
J B, Summers, H, Mazdiyasni, J H, Holms, J D, Ratajczyk, R D, Dyer, G W, Carter   +5 more
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15-Lipoxygenase inhibitors: a patent review

Expert Opinion on Therapeutic Patents, 2015
15-Lipoxygenases (15-LOXes) are a family of iron-containing proteins that have the capability for unsaturated fatty acid peroxidation in animals and plants. Two types of the enzyme, 15-LOX-1 and 15-LOX-2, have been recognized in mammals to have different abilities in the peroxidation of arachidonic acid and linoleic acid.
Hamid, Sadeghian, Atena, Jabbari
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4-Hydroxythiazole inhibitors of 5-lipoxygenase

Journal of Medicinal Chemistry, 1991
4-Hydroxythiazoles have been identified as potent inhibitors of 5-lipoxygenase in vitro exhibiting IC50's of less than 1 microM. An investigation of structure-activity relationships showed that the most potent inhibitors of this series are the 5-phenyl derivatives. The corresponding thiazolidin-4-one analogues were found to be relatively inactive.
F A, Kerdesky, J H, Holms, J L, Moore, R L, Bell, R D, Dyer, G W, Carter, D W, Brooks   +6 more
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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, Divakar K C, Sekhar, Rao A G, Appu, N G, Karanth, A P, Sattur   +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, C D, Brooks, K I, Hulkower, J B, Bouska, R L, Bell   +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, S. Divakar, A.G. Appu Rao, N.G. Karanth, A.P. Sattur   +4 more
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