title: Synthesis and pharmacochemical study of novel polyfunctional molecules combining anti-inflammatory, antioxidant, and hypocholesterolemic properties.
abstract: 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.
authors.affiliation: Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, 541 24 Thessaloniki, Greece.
authors.forename: Christos M
authors.initials: CM
authors.lastname: Doulgkeris
authors.forename: Dimitrios
authors.initials: D
authors.lastname: Galanakis
authors.forename: Angeliki P
authors.initials: AP
authors.lastname: Kourounakis
authors.forename: Karyofyllis C
authors.initials: KC
authors.lastname: Tsiakitzis
authors.forename: Antonios M
authors.initials: AM
authors.lastname: Gavalas
authors.forename: Phaedra T
authors.initials: PT
authors.lastname: Eleftheriou
authors.forename: Panagiotis
authors.initials: P
authors.lastname: Victoratos
authors.forename: Eleni A
authors.initials: EA
authors.lastname: Rekka
authors.forename: Panos N
authors.initials: PN
authors.lastname: Kourounakis
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D000924:Anticholesteremic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D000975:Antioxidants / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001168:Arthritis / Q000188:drug therapy*; D002784:Cholesterol / Q000097:blood; D004195:Disease Models, Animal; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D005260:Female; D007249:Inflammation / Q000188:drug therapy*; D010875:Pipecolic Acids / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011392:Proline / Q000031:analogs & derivatives / Q000138:chemical synthesis / Q000494:pharmacology*; D051381:Rats; D011916:Rats, Inbred F344; D013329:Structure-Activity Relationship; D014280:Triglycerides / Q000097:blood
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D000924:Anticholesteremic Agents; D000975:Antioxidants; D010875:Pipecolic Acids; D014280:Triglycerides; D002784:Cholesterol; D011392:Proline