Synthesis and pharmacochemical study of novel polyfunctional molecules combining anti-inflammatory, antioxidant, and hypocholesterolemic properties
R = Indomethacin or naproxen residue; Q = CH 2, CHOH or (CH 2) 2; X = H or COOC 2H 5. 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-...
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Veröffentlicht in: | Bioorganic & medicinal chemistry letters 2006-02, Vol.16 (4), p.825-829 |
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Hauptverfasser: | , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
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Zusammenfassung: | R
=
Indomethacin or naproxen residue; Q
=
CH
2, CHOH or (CH
2)
2; X
=
H or COOC
2H
5.
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. |
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ISSN: | 0960-894X 1464-3405 |
DOI: | 10.1016/j.bmcl.2005.11.027 |