Open AccessSynthesis and Preliminary Pharmacological Evaluation of Aminobenzensulfonamides Derivatives of Mefenamic Acid as a Potential Anti-inflammatory Agents
Author(s) -
Monther F. Mahdi
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/vol17iss1pp7-15
Subject(s) - mefenamic acid , pharmacology , diclofenac sodium , chemistry , diclofenac , pharmacophore , edema , in vivo , anti inflammatory , nonsteroidal , salicylamide , ibuprofen , medicine , biochemistry , organic chemistry , microbiology and biotechnology , biology
A group of amino derivatives [4-aminobenzenesulfonamide,4-amino-N¹ methylbenzenesulfonamide, or N¹-(4-aminophenylsulfonyl)acetamide] bound to carboxyl group of mefenamic acid a well known nonsteroidal anti-inflammatory drugs (NSAIDs) were designed and synthesized for evaluation as a potential anti-inflammatory agent. In vivo acute anti-inflammatory activity of the final compounds (9, 10 and 11) was evaluated in rat using egg-white induced edema model of inflammation in a dose equivalent to (7.5mg/Kg) of mefenamic acid. 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-amino-N-methylbenzenesulfonamide derivative (compound 10) exhibited comparable anti-inflammatory activity to diclofenac (3mg/Kg) at times 180-300 minute with the same onset of action. The results of this study indicate that the incorporation of the 4-aminobenzenesulfonamide pharmacophore and its derivatives in to mefenamic acid maintain its anti-inflammatory activity.
Key ward: benzenesulfonamide, anti-inflammatory, paw edema, NSAIDs, mefenamic acid