Τίτλος:
Design and study of some novel ibuprofen derivatives with potential nootropic and neuroprotective properties
Γλώσσες Τεκμηρίου:
Αγγλικά
Περίληψη:
Six novel ibuprofen derivatives and related structures, incorporating a proline moiety and designed for neurodegenerative disorders, are studied. They possess anti-inflammatory properties and three of them inhibited lipoxygenase. One compound was found to inhibit cyclooxygenase (COX)-2 production in spleenocytes from arthritic rats. The HS-containing compounds are potent antioxidants and one of them protected against glutathione loss after cerebral ischemia/reperfusion. They demonstrated lipid-lowering ability and seem to acquire low gastrointestinal toxicity. Acetylcholinesterase inhibitory activity, found in two of these compounds, may be an asset to their actions. © 2006 Elsevier Ltd. All rights reserved.
Συγγραφείς:
Siskou, I.C.
Rekka, E.A.
Kourounakis, A.P.
Chrysselis, M.C.
Tsiakitzis, K.
Kourounakis, P.N.
Περιοδικό:
BIOORGANIC AND MEDICINAL CHEMISTRY
Λέξεις-κλειδιά:
1 [2 (4 isobutylphenyl)propanoyl] n (2 mercaptoethyl)pyrrolidine 2 carboxamide; 2 methoxy 4 methylphenyl 1 (isobutyryl)pyrrolidine 2 carboxylate; 2 methoxy 4 methylphenyl 1 [2 (4 isobutylphenyl)propanoyl]pyrrolidine 2 carboxylate; 3 (pyridin 3 yl)propyl 1 (isobutyryl)pyrrolidine 2 carboxylate; 3 (pyridin 3 yl)propyl 1 [2 (4 isobutylphenyl)propanoyl]pyrrolidine 2 carboxylate; acetylcholinesterase; antioxidant; cyclooxygenase 2; ethyl 2 [1 [2 (4 isobutylphenyl)propanoyl]pyrrolidine 2 carboxamido] 3 mercaptopropanoate; glutathione; ibuprofen; ibuprofen derivative; lipoxygenase, adjuvant arthritis; animal cell; animal experiment; animal model; animal tissue; antiinflammatory activity; arthritis; article; brain ischemia; brain perfusion; controlled study; degenerative disease; drug design; enzyme synthesis; gastrointestinal toxicity; male; mouse; neuroprotection; nonhuman; paw edema; rat; reperfusion injury, Animals; Antioxidants; Arthritis, Experimental; Blood-Brain Barrier; Cholesterol; Cholinesterase Inhibitors; Cyclooxygenase 2 Inhibitors; Freund's Adjuvant; Gastrointestinal Diseases; Glutathione; Hyperlipidemias; Hypoxia-Ischemia, Brain; Ibuprofen; Lipid Peroxidation; Lipoxygenase Inhibitors; Mice; Microsomes, Liver; Neuroprotective Agents; Nootropic Agents; Oxidative Stress; Picrates; Rats; Spleen; Triglycerides
DOI:
10.1016/j.bmc.2006.10.056
