Table 4.

In vitro COX-1/COX-2 inhibition (IC₅₀, μmol/L), selectivity index and in vivo anti-inflammation activity (dose = 150 μmol/kg) for compounds 52–55, and standard agents.

Compd.	COX-1a	COX-2a	COX-2 selectivityb	Rat paw edema (% edema inhibition, 5 h)
52	54.99	0.74	74.31	41.06 ± 2.64
53	63.76	0.48	132.83	58.04 ± 1.30
54	55.05	0.81	67.96	46.38 ± 2.47
55	60.61	0.89	68.10	59.33 ± 2.19
Celecoxib	37.98	0.10	379.80	49.81 ± 1.92
Indomethacin	98.23	50.99	‒	‒

^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).