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https://hdl.handle.net/20.500.14279/30370
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 |
Εμφανίζεται στις συλλογές: | Άρθρα/Articles |
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molecules-27-02104-v2.pdf | Full text | 2.1 MB | Adobe PDF | Δείτε/ Ανοίξτε |
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