Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 31, Issue -, Pages 54-60Publisher
TAYLOR & FRANCIS LTD
DOI: 10.1080/14756366.2016.1201815
Keywords
Anti-inflammatory; cyclooxygenase-2 inhibitors; 1; 5-diarylpyrazole
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A new series of 1,5-diarylpyrazoles 10a-l was designed and synthesized for evaluation as COX inhibitors and as anti-inflammatory agents. All compounds were more selective for COX-2 isozyme and showed good in vivo anti-inflammatory activity. Compound 10e was the most COX-2 selective compound (S.I.=10.67) and the most potent anti-inflammatory derivative (ED50=46mol/kg) which is approximately 11-folds more potent than ibuprofen (ED50=499mol/kg) and had 2/3 potency of celecoxib (ED50=31mol/kg). All compounds were less ulcerogenic (ulcer indexes=1.20-4.61) than ibuprofen (ulcer index=20.25) and comparable to celecoxib (ulcer index=2.90).
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