Synthesis and pharmacochemical study of novel polyfunctional molecules combining anti-inflammatory, antioxidant, and hypocholesterolemic properties

被引:26
作者
Doulgkeris, CM
Galanakis, D
Kourounakis, AP
Tsiakitzis, KC
Gavalas, AM
Eleftheriou, PT
Victoratos, P
Rekka, EA
Kourounakis, PN [1 ]
机构
[1] Aristotle Univ Thessaloniki, Sch Pharm, Dept Pharmaceut Sci, Thessaloniki 54124, Greece
[2] Papageorgiou Gen Hosp, Dept Pharm, Thessaloniki 56403, Greece
[3] Univ Athens, Sch Pharm, Dept Pharmaceut Chem, GR-15771 Athens, Greece
[4] Aristotle Univ Thessaloniki, Fac Sci, Sch Biol, Dept Genet Dev & Mol Biol, Thessaloniki 54124, Greece
关键词
neurodegeneration; L-cysteine; NSAIDs; proline amide conjugates; antioxidants; anti inflammatories; lipoxygenase; hypocholesterolemics; gastrointestinal toxicity;
D O I
10.1016/j.bmcl.2005.11.027
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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, frans-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. (c) 2005 Elsevier Ltd. All rights reserved.
引用
收藏
页码:825 / 829
页数:5
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