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Doulgkeris CM Galanakis D Kourounakis AP Tsiakitzis KC Gavalas AM Eleftheriou PT Victoratos P Rekka EA Kourounakis PN 《Bioorganic & medicinal chemistry letters》2006,16(4):825-829
We have designed and synthesized a series of novel molecules having a residue of a classical NSAID and an antioxidant moiety, both attached through amide bonds to a known nootropic structure, an L-proline, trans-4-hydroxy-L-proline or DL-pipecolinic acid residue. The compounds were found to retain anti-inflammatory and antioxidant activities, to acquire hypocholesterolemic action, and to possess a greatly reduced gastrointestinal toxicity. The novel molecules could find useful applications, among others, in slowing the progression or delaying the onset of neurodegenerative diseases. 相似文献
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Ziakas GN Rekka EA Gavalas AM Eleftheriou PT Tsiakitzis KC Kourounakis PN 《Bioorganic & medicinal chemistry》2005,13(23):6485-6492
Tolfenamic acid esters with nitrooxyalcohols are synthesized. They are anti-inflammatory agents reducing carrageenan rat paw edema, with low gastrointestinal and general toxicity. In vitro, they are nitric oxide donors, inhibitors of lipoxygenase and cyclooxygenases. A two to three carbon chain between carboxylic and nitric ester groups seems optimal for activity. 相似文献
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Galanakis D Kourounakis AP Tsiakitzis KC Doulgkeris C Rekka EA Gavalas A Kravaritou C Charitos C Kourounakis PN 《Bioorganic & medicinal chemistry letters》2004,14(14):3639-3643
The synthesis and pharmacological evaluation of a series of amide derivatives of NSAIDs with L-cysteine ethyl ester is described. The novel derivatives are potent antiinflammatory, antioxidant and hypocholesterolemic-hypolipidemic agents, while they demonstrate considerably reduced gastrointestinal toxicity. This molecular modification may offer a general route to safer antiinflammatory agents, potentially suitable for chronic use in conditions such as neurodegenerative disorders. 相似文献
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Siskou IC Rekka EA Kourounakis AP Chrysselis MC Tsiakitzis K Kourounakis PN 《Bioorganic & medicinal chemistry》2007,15(2):951-961
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. 相似文献
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