Τίτλος:
Synthesis and pharmacochemical study of novel polyfunctional molecules combining anti-inflammatory, antioxidant, and hypocholesterolemic properties
Γλώσσες Τεκμηρίου:
Αγγλικά
Περίληψη:
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. © 2005 Elsevier Ltd. All rights reserved.
Συγγραφείς:
Doulgkeris, C.M.
Galanakis, D.
Kourounakis, A.P.
Tsiakitzis, K.C.
Gavalas, A.M.
Eleftheriou, P.T.
Victoratos, P.
Rekka, E.A.
Kourounakis, P.N.
Περιοδικό:
Bioorganic and Medicinal Chemistry Letters
Λέξεις-κλειδιά:
amide; hydroxyproline; hypocholesterolemic agent; nonsteroid antiinflammatory agent; nootropic agent; pipecolic acid; polyfunctional group; proline, amidation; animal cell; animal experiment; animal model; antiinflammatory activity; antioxidant activity; arthritis; article; controlled study; degenerative disease; drug synthesis; female; gastrointestinal toxicity; in vitro study; in vivo study; lipid peroxidation; nonhuman; rat, Animals; Anti-Inflammatory Agents, Non-Steroidal; Anticholesteremic Agents; Antioxidants; Arthritis; Cholesterol; Disease Models, Animal; Drug Design; Drug Evaluation, Preclinical; Female; Inflammation; Pipecolic Acids; Proline; Rats; Rats, Inbred F344; Structure-Activity Relationship; Triglycerides, Animalia
DOI:
10.1016/j.bmcl.2005.11.027
