Table 3.

In vitro COX-1/COX-2 inhibition (IC₅₀, μmol/L), selectivity index, ulcerogenic evaluation and in vivo anti-inflammation activity (dose = 50 mg/kg) for compounds 39‒44, and standard agents.

Compd.	COX-1a	COX-2a	COX-2 selectivityb	Ulcer index	Rat paw edema (mm) (% edema inhibition, 6 h)
39	11.3	0.045	251.11	0.21 ± 0.02	7.27 ± 0.14
40	12.4	0.041	302.44	0.123 ± 0.01	5.10 ± 0.36
41	10.5	0.064	164.06	0.26 ± 0.01	6.54 ± 0.0.14
42	12.8	0.043	297.67	0.21 ± 0.01	5.47 ± 0.23
43	10.9	0.065	167.69	0.55 ± 0.03	7.05 ± 0.35
44	12.4	0.039	317.95	0.11 ± 0.01	4.99 ± 0.19
Celecoxib	12.7	0.045	282.22	0.167 ± 0.01	5.21 ± 0.19
Indomethacin	0.10	0.080	1.25	0.88 ± 0.04	‒

‒Not applicable.

^aThe result (IC₅₀, μmol/L) is the mean of three determinations acquired using a COX fluorescent inhibitor screening assay kit (Cayman Chemical, MI, USA).

^bCOX-2 selectivity index (COX-1 IC₅₀/COX-2 IC₅₀).