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Τίτλος: Enhancement of the Anti-Inflammatory Activity of NSAIDs by Their Conjugation with 3,4,5-Trimethoxybenzyl Alcohol
Συγγραφείς: Tziona, Paraskevi 
Theodosis-Nobelos, Panagiotis 
Papagiouvannis, Georgios 
Petrou, Anthi 
Drouza, Chryssoula 
Rekka, Eleni A 
Major Field of Science: Engineering and Technology
Field Category: Environmental Biotechnology
Λέξεις-κλειδιά: anti-inflammatory derivatives;cyclooxygenase inhibition;lipoxygenase inhibition;molecular docking;non steroidal anti-inflammatory drugs
Ημερομηνία Έκδοσης: 24-Μαρ-2022
Πηγή: Molecules, 2022, vol. 27, iss. 7
Volume: 27
Issue: 7
Περιοδικό: Molecules 
Περίληψη: The synthesis of derivatives of three nonspecific COX-1 and COX-2 inhibitors, ibuprofen, ketoprofen, naproxen is presented. These acids were connected via an amide bond with an amino acid (L-proline, L-tyrosine, and beta-alanine) used as a linker. The amino acid carboxylic group was esterified with 3,4,5 trimethoxybenzyl alcohol. The activity of the novel derivatives was examined in vivo on carrageenan-induced inflammation, and in vitro, as cyclooxygenase and lipoxygenase inhibitors. It was found that the new compounds were more potent anti-inflammatory agents than the parent drugs. Thus, the ibuprofen (21) and ketoprofen (16) derivatives reduced rat paw edema by 67 and 91% (the reduction by the relevant NSAIDs was 36 and 47%, respectively). They inhibited COX-2 more than the starting drugs (21 by 67%, ibuprofen 46%, 19 by 94%, ketoprofen 49%). Docking of compounds on the active sites of COX-1 and COX-2 reflects their in vitro activity. Thus, 19 adopts an unfavorable orientation for COX-1 inhibition, but it binds effectively in the binding pocket of COX-2, in agreement with the absence of activity for COX-1 and the high inhibition of COX-2. In conclusion, the performed structural modifications result in the enhancement of the anti-inflammatory activity, compared with the parent NSAIDs.
URI: https://hdl.handle.net/20.500.14279/30370
ISSN: 14203049
DOI: 10.3390/molecules27072104
Rights: © by the authors
Attribution-NonCommercial-NoDerivatives 4.0 International
Type: Article
Affiliation: Aristotle University of Thessaloniki 
Frederick University 
Cyprus University of Technology 
Publication Type: Peer Reviewed
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