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

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.

Graphical abstractR = Indomethacin or naproxen residue; Q = CH2, CHOH or (CH2)2; X = H or COOC2H5.Figure optionsDownload full-size imageDownload as PowerPoint slide