1.Synthesis and pharmacochemical study of novel polyfunctional molecules combining anti-inflammatory, antioxidant, and hypocholesterolemic properties.
Doulgkeris CM1, Galanakis D, Kourounakis AP, Tsiakitzis KC, Gavalas AM, Eleftheriou PT, Victoratos P, Rekka EA, Kourounakis PN. Bioorg Med Chem Lett. 2006 Feb 15;16(4):825-9. Epub 2005 Nov 23.
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.