Synthesis and Preliminary Pharmacological Evaluation of New Analogues of Diclofenac as Potential Anti-inflammatory Agents
A group of amine derivatives [4-aminobenzenesulfonamide derivatives, 2-aminopyridine and 2-aminothiazole] incorporated to α-carbon of diclofenac a well known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were designed and synthesized for evaluation as a potential ant...
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| Format: | Article |
| Language: | English |
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College of Pharmacy University of Baghdad
2017-03-01
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| Series: | Iraqi Journal of Pharmaceutical Sciences |
| Online Access: | https://www.bijps.uobaghdad.edu.iq/index.php/bijps/article/view/489 |
| _version_ | 1797317299370196992 |
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| author | Noor H. Naser Monther F. Mahdi Tagreed N-A Omar Amar A. Fadhil |
| author_facet | Noor H. Naser Monther F. Mahdi Tagreed N-A Omar Amar A. Fadhil |
| author_sort | Noor H. Naser |
| collection | DOAJ |
| description |
A group of amine derivatives [4-aminobenzenesulfonamide derivatives, 2-aminopyridine and 2-aminothiazole] incorporated to α-carbon of diclofenac a well known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were designed and synthesized for evaluation as a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of the selected final compounds (9, 12 and 13) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (3 mg/Kg) of diclofenac sodium. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the 4-aminobenzenesulfonamide derivative (compound 9) exhibited superior anti-inflammatory activity compared to diclofenac sodium at times 180-300 minutes with the same onset of action. The results of this study indicate that the incorporation of the selected aromatic amino groups in to diclofenac maintain its anti-inflammatory activity.
Key words: amine derivatives, anti-inflammatory, diclofenac derivatives, COX-2 selectivity.
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| first_indexed | 2024-03-08T03:32:54Z |
| format | Article |
| id | doaj.art-166bc4d44acd45f58a075f47b2c42381 |
| institution | Directory Open Access Journal |
| issn | 1683-3597 2521-3512 |
| language | English |
| last_indexed | 2024-03-08T03:32:54Z |
| publishDate | 2017-03-01 |
| publisher | College of Pharmacy University of Baghdad |
| record_format | Article |
| series | Iraqi Journal of Pharmaceutical Sciences |
| spelling | doaj.art-166bc4d44acd45f58a075f47b2c423812024-02-10T10:58:06ZengCollege of Pharmacy University of BaghdadIraqi Journal of Pharmaceutical Sciences1683-35972521-35122017-03-0120110.31351/vol20iss1pp25-32Synthesis and Preliminary Pharmacological Evaluation of New Analogues of Diclofenac as Potential Anti-inflammatory AgentsNoor H. NaserMonther F. MahdiTagreed N-A OmarAmar A. Fadhil A group of amine derivatives [4-aminobenzenesulfonamide derivatives, 2-aminopyridine and 2-aminothiazole] incorporated to α-carbon of diclofenac a well known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were designed and synthesized for evaluation as a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of the selected final compounds (9, 12 and 13) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (3 mg/Kg) of diclofenac sodium. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the 4-aminobenzenesulfonamide derivative (compound 9) exhibited superior anti-inflammatory activity compared to diclofenac sodium at times 180-300 minutes with the same onset of action. The results of this study indicate that the incorporation of the selected aromatic amino groups in to diclofenac maintain its anti-inflammatory activity. Key words: amine derivatives, anti-inflammatory, diclofenac derivatives, COX-2 selectivity. https://www.bijps.uobaghdad.edu.iq/index.php/bijps/article/view/489 |
| spellingShingle | Noor H. Naser Monther F. Mahdi Tagreed N-A Omar Amar A. Fadhil Synthesis and Preliminary Pharmacological Evaluation of New Analogues of Diclofenac as Potential Anti-inflammatory Agents Iraqi Journal of Pharmaceutical Sciences |
| title | Synthesis and Preliminary Pharmacological Evaluation of New Analogues of Diclofenac as Potential Anti-inflammatory Agents |
| title_full | Synthesis and Preliminary Pharmacological Evaluation of New Analogues of Diclofenac as Potential Anti-inflammatory Agents |
| title_fullStr | Synthesis and Preliminary Pharmacological Evaluation of New Analogues of Diclofenac as Potential Anti-inflammatory Agents |
| title_full_unstemmed | Synthesis and Preliminary Pharmacological Evaluation of New Analogues of Diclofenac as Potential Anti-inflammatory Agents |
| title_short | Synthesis and Preliminary Pharmacological Evaluation of New Analogues of Diclofenac as Potential Anti-inflammatory Agents |
| title_sort | synthesis and preliminary pharmacological evaluation of new analogues of diclofenac as potential anti inflammatory agents |
| url | https://www.bijps.uobaghdad.edu.iq/index.php/bijps/article/view/489 |
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