Synthesis, characterization and preliminary pharmacological evaluation of new non-steroidal anti-inflammatory pyrazoline derivatives

Abstract

A series of six pyrazoline ring derivatives as a pharmacophore were incorporated to the naproxen; to increase its size were synthesized and preliminarly evaluated as anti-inflammatory agents with expected selectivity toward COX-2 enzyme. In vivo acute anti-inflammatory effects of the final compounds (5a-f) were evaluated in rats using egg-white induced edema model of inflammation. The tested compounds and the reference drug (naproxen) produced significant reduction of paw edema with respect to the effect of control group (propylene glycol 50%, v:v). However, compound 5d and 5e show comparable effect to naproxen at all experimental time while compounds 5a, 5b and 5c produced significantly lower inhibitory effect than naproxen at time 120-240 minutes. Furthermore, compound 5f exert significantly higher paw edema reduction than naproxen at 60-240 min. Also the antibacterial activities of the final compounds were evaluated by Well Diffusion Method. All tested compounds exert significant antibacterial activity against tested Gram positive and Gram negative bacteria in comparison to dimethyl sulfoxide as control group. In comparison the antibacterial results among the tested compound 5e may regard the best one and compound 5c the lower one.