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Five groups of diarylheterocycles with a central pyrazole ring (12a–d), pyrazoline ring (14a–d), or pyridine ring (15a–d, 16a–d and 17a–d) were synthesized and evaluated in vitro for COX-1/COX-2 inhibitory activity and in vivo for anti-inflammatory activity. All compounds that possessed anti-inflammatory activity were assessed for their ulcerogenic liability in comparison with ibuprofen and celecoxib. The pyrazole derivative 12b and the pyrazoline derivative 14b were the least ulcerogenic compounds with relative ulcerogenicities to celecoxib 0.85 and 0.90 respectively.