Green synthesis and biological screening of some fluorinated pyrazole chalcones in search of potent anti-inflammatory and analgesic agents | ||
| Egyptian Pharmaceutical Journal | ||
| Volume 19, Issue 2, April 2020, Pages 172-181 PDF (2.28 M) | ||
| DOI: 10.4103/epj.epj_64_19 | ||
| Authors | ||
| Shravan Y. Jadhav; Nargisbano A. Peerzade; Rakhi G. Gawali; Raghunath B. Bhosale; Amol A. Kulkarni; Bhushan D. Varpe | ||
| Abstract | ||
| Background and objective Fluorinated pyrazoles are widely studied for their anti-inflammatory activities. A new series of fluorinated pyrazole chalcones ( and ) were synthesized and screened for anti-inflammatory and analgesic activities. Materials and methods Fluorinated pyrazole chalcones were synthesized using polyethylene glycol 400 (PEG-400) as an alternative reaction medium. The anti-inflammatory activity of compounds and were assessed by the carrageenan paw edema model in rats. Analgesic activity was studied by the tail-flick method in rats. Result and conclusion Among the series, compound was found to be the most potent anti-inflammatory agent, whereas compounds ,,,,,, and showed significant anti-inflammatory activity comparable to the reference standard diclofenac sodium. Three compounds ,, and showed significant analgesic activity comparable to the reference standard aspirin. From the result, compounds ,,,, and have found biologically active members with an interesting dual anti-inflammatory and analgesic profile. Anti-inflammatory activities are supported by the docking study to analyze the possible interactions with the cyclooxygenase-2 enzyme. | ||
| Keywords | ||
| ADME; analgesic activity; Anti-inflammatory; Molecular docking; PEG-400; pyrazole chalcones | ||
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