Zobrazeno 1 - 10
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pro vyhledávání: '"Alwine Schulze Elfringhoff"'
Publikováno v:
European Journal of Medicinal Chemistry. 125:1107-1114
Cytosolic phospholipase A2α (cPLA2α) is a key enzyme in the biosynthesis of pro-inflammatory lipid mediators and therefore represents an attractive target for the development of new anti-inflammatory drugs. Recently, we have found that 1-[3-(4-octy
Publikováno v:
European journal of medicinal chemistry. 125
Cytosolic phospholipase A
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 21:1773-1776
Indole-5-carboxylic acids with 3-aryloxy-2-oxopropyl residues in position 1 have been found to be potent inhibitors of human cytosolic phospholipase A2α (cPLA2α). In course of structure–activity relationship studies, we investigated the effect of
Publikováno v:
ChemMedChem. 6:544-549
Cytosolic phospholipase A2α (cPLA2α) and fatty acid amide hydrolase (FAAH) are enzymes that have emerged as attractive targets for the development of analgesic and anti-inflammatory drugs. We recently reported that 1-[3-(4-octylphenoxy)-2-oxopropyl
Publikováno v:
Analytical and Bioanalytical Chemistry. 394:1679-1685
A fluorescent assay for the evaluation of inhibitors of fatty acid amide hydrolase (FAAH) is described. Microsomes from rat brain served as enzyme source. N-(2-Hydroxyethyl)-4-pyren-1-ylbutanamide was designed and synthesized as novel fluorogenic sub
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:2107-2111
The indole ring systems of the cytosolic phospholipase A(2)alpha (cPLA(2)alpha) inhibitor 1-[3-(4-octylphenoxy)-2-oxopropyl]indole-5-carboxylic acid (2) and the isomeric 6-carboxylic acid (3) were replaced by benzimidazole, benzotriazole and indazole
Publikováno v:
Bioorganic & Medicinal Chemistry. 15:2883-2891
Indole-5-carboxylic acids and -carboxamides with 3-aryloxy-2-oxopropyl residues in position 1 were previously reported to be potent inhibitors of cytosolic phospholipase A(2)alpha (cPLA(2)alpha) isolated from human platelets. In continuation of our a
Autor:
and Alwine Schulze Elfringhoff, Stefanie Bovens, Joachim Ludwig, Carsten Brauch, Matthias Lehr
Publikováno v:
Journal of Medicinal Chemistry. 49:2611-2620
The synthesis and structure-activity relationship study of a series of 1-indol-1-yl-3-phenoxypropan-2-one inhibitors of cytosolic phospholipase A(2)alpha (cPLA(2)alpha) are described. The compounds were evaluated in a vesicle assay with isolated cPLA
Publikováno v:
Journal of Enzyme Inhibition and Medicinal Chemistry. 20:429-437
Recently we found that 1-methyldodecanoylindole-2-carboxylic acid (1) and 1-[2-(4-carboxyphenoxy)ethyl]-3-dodecanoylindole-2-carboxylic acid (4) were inhibitors of the cytosolic phospholipase A2alpha (cPLA2alpha)-mediated arachidonic acid release in
Publikováno v:
Journal of Chromatography B. 769:185-190
A procedure for the determination of the influence of detergents on the cell integrity of human platelets by measuring the release of serotonin with high-performance liquid chromatography and fluorescence detection is presented. After exposure of the