Novel Pyrazole Derivatives as Potential Promising Anti‐inflammatory Antimicrobial Agents

Abstract

Four series of 1H‐pyrazole derivatives have been synthesized. The first series was synthesized starting by condensing the hydrazine derivatives 1a–d with 4‐(1‐ethoxycarbonyl‐2‐oxopropyl)azobenzoic acid 2a in ethanol or glacial acetic acid to generate the corresponding pyrazoline derivatives 3a–d. Likewise, heating 1a–d with 4‐(1‐acetyl‐2‐oxopropyl)azobenzoic acid 2b gave rise to the pyrazole derivatives 4a–d. Similarly, reaction of 1a–d with ethyl 2‐(1,5‐dimethyl‐3‐oxo‐2‐phenyl‐2,3‐dihydro‐1Hpyrazol‐4‐ylazo)‐3‐oxobutanoate 2c or 3‐(1,5‐dimethyl‐3‐oxo‐2‐phenyl‐2,3‐dihydro‐1H‐pyrazol‐4‐yl azo)pentane‐2,4‐dione 2d in ethanol or glacial acetic acid led to the corresponding pyrazoline derivatives 5a–d or pyrazole derivatives 6a–d. The newly synthesized compounds were evaluated for their anti‐inflammatory‐antimicrobial activities. In addition, the ulcerogenic and acute toxicity profiles were determined. Compound 6c, proved to be the most active anti‐inflammatory‐antimicrobial agent in the present study with a good safety margin and no ulcerogenic effect.