Open AccessSynthesis and Preliminary Pharmacological Evaluation of New Analogues of Diclofenac as Potential Anti-inflammatory Agents
Author(s) -
Noor H. Naser,
Monther F. Mahdi,
Tagreed N-A Omar,
Amar A. Fadhil
Publication year - 2017
Publication title -
al-maǧallaẗ al-’irāqiyyaẗ li-l-’ulūm al-ṣaydalāniyyaẗ/iraqi journal of pharmaceutical sciences
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.122
H-Index - 1
eISSN - 2521-3512
pISSN - 1683-3597
DOI - 10.31351/vol20iss1pp25-32
Subject(s) - diclofenac sodium , diclofenac , chemistry , selectivity , pharmacology , anti inflammatory , edema , amine gas treating , in vivo , drug , medicine , organic chemistry , chromatography , biochemistry , catalysis , surgery , microbiology and biotechnology , biology
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.