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.
Doulgkeris
Christos M
CM
Department of Pharmaceutical Chemistry, School of Pharmacy, Aristotelian University of Thessaloniki, 541 24 Thessaloniki, Greece.
Galanakis
Dimitrios
D
Kourounakis
Angeliki P
AP
Tsiakitzis
Karyofyllis C
KC
Gavalas
Antonios M
AM
Eleftheriou
Phaedra T
PT
Victoratos
Panagiotis
P
Rekka
Eleni A
EA
Kourounakis
Panos N
PN
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
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000924:Anticholesteremic Agents; D000975:Antioxidants; D010875:Pipecolic Acids; D014280:Triglycerides; D002784:Cholesterol; D011392:Proline