Synthesis and Biological Evaluation of New Diarylpyrazole and Triarylimidazoline Derivatives as Selective COX ‐2 Inhibitors

New series of diarylpyrazoles 8a–f and triarylimidazoline‐5‐ones 11a–g were synthesized and evaluated for their in vitro cyclooxygenase‐1 (COX‐1) and COX‐2 inhibitory activity and in vivo anti‐inflammatory activity. The synthesized compounds showed good selectivity for COX‐2; compounds 8a, 8d, 8f, 11a, and 11c exhibited the highest COX‐2 selectivity indexes (SI = 4.77–5.43) compared to the reference drug celecoxib (SI = 7.8). All compounds showed good in vivo anti‐inflammatory activity, especially compounds 8a, 8f, 11c, and 11d, which also showed some similarities to the time interval pattern of celecoxib at all different time intervals (1, 3, and 6 h). New series of diarylpyrazoles (8a–f) and triarylimidazoline‐5‐ones (11a–g) were synthesized and evaluated for their in vitro cyclooxygenase‐1/2 (COX‐1/2)‐inhibitory and in vivo anti‐inflammatory activities. Compounds 8a, 8d, 8f, 11a, and 11c exhibited the highest COX‐2 selectivity (SI = 4.77–5.43) compared to celecoxib (SI = 7.8) and all compounds showed good in vivo anti‐inflammatory activity.
Source: Archiv der Pharmazie - Category: Drugs & Pharmacology Authors: Tags: Full Paper Source Type: research