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
相关论文
共 50 条
  • [1] Synthesis and pharmacological evaluation of polyfunctional benzimidazole-NSAID chimeric molecules combining anti-inflammatory, immunomodulatory and antioxidant activities
    Bansal, Yogita
    Silakari, Om
    ARCHIVES OF PHARMACAL RESEARCH, 2014, 37 (11) : 1426 - 1436
  • [2] Synthesis and pharmacological evaluation of polyfunctional benzimidazole-NSAID chimeric molecules combining anti-inflammatory, immunomodulatory and antioxidant activities
    Yogita Bansal
    Om Silakari
    Archives of Pharmacal Research, 2014, 37 : 1426 - 1436
  • [3] Design and Synthesis of Novel Anti-inflammatory/Anti-ulcer Hybrid Molecules with Antioxidant Activity
    Chaudhari, Bhim Bahadur
    Bali, Alka
    Balaini, Ajitesh
    MEDICINAL CHEMISTRY, 2021, 17 (09) : 994 - 1006
  • [4] Novel polyfunctional hypocholeterolemic, anti-inflammatory and antioxidant compounds and prospective nootropic agents
    Doulgkeris, C
    Kourounakis, AP
    Tsiakitzis, K
    Galanakis, D
    Rekka, EA
    Kourounakis, PN
    CHEMISTRY AND PHYSICS OF LIPIDS, 2005, 136 (02) : 160 - 161
  • [5] Synthesis and pharmacological evaluation of novel derivatives of anti-inflammatory drugs with increased antioxidant and anti-inflammatory activities
    Kourounakis, AP
    Galanakis, D
    Tsiakitzis, K
    Rekka, EA
    Kourounakis, PN
    DRUG DEVELOPMENT RESEARCH, 1999, 47 (01) : 9 - 16
  • [6] Antioxidant and anti-inflammatory properties of curcumin
    Menon, Venugopal P.
    Sudheer, Adluri Ram
    MOLECULAR TARGETS AND THERAPEUTIC USES OF CURCUMIN IN HEALTH AND DISEASE, 2007, 595 : 105 - 125
  • [7] Synthesis and pharmacochemical evaluation of novel aryl-acetic acid inhibitors of lipoxygenase, antioxidants, and anti-inflammatory agents
    Pontiki, E.
    Hadjipavlou-Litina, D.
    BIOORGANIC & MEDICINAL CHEMISTRY, 2007, 15 (17) : 5819 - 5827
  • [8] Novel 1,2,4-triazole-3-acetate derivatives combining anti-inflammatory and antioxidant properties
    Poptsis, A.
    Rekka, E. A.
    Kourounakis, P. N.
    FREE RADICAL RESEARCH, 2009, 43 : 95 - 95
  • [9] Synthesis, Antioxidant and Anti-inflammatory Properties of an Apocynin- Derived Dihydrocoumarin
    Paracatu, Luana C.
    Zeraik, Maria L.
    Bertozo, Luiza de Carvalho
    Bartolomeu, Aloisio de Andrade
    da Silva Filho, Luiz C.
    da Fonseca, Luiz M.
    Ximenes, Valdecir F.
    MEDICINAL CHEMISTRY, 2017, 13 (01) : 93 - 100
  • [10] Anti-inflammatory, analgesic and antioxidant activities of novel kyotorphin-nitroxide hybrid molecules
    Bi, Wei
    Bi, Yue
    Gao, Xiang
    Yan, Xin
    Zhang, Yanrong
    Xue, Ping
    Bammert, Catherine E.
    Legalley, Thomas D.
    Gibson, K. Michael
    Bi, Lanrong
    Wang, Jia-Xiang
    BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2016, 26 (08) : 2005 - 2013