Table 7.

Metabolic Stability and CYP450 Inhibition of Selected Derivatives.

#	Metabolic Stability (% Remaining)a				CYP450 Isoforms Inhibition %b
	Plasma		Liver Microsome		1A2	2C9	2D6	3A4
	Human	Mouse	Human	Mouse
20	100	85	79	64	7	45	0	0
22	100	100	100	37	1	39	11	0
25	100	100	100	70	0	16	14	2
27	100	100	100	76	6	88	7	24
29	100	100	10	42	11	100	6	0
31	100	100	100	51	40	55	23	41
33	100	100	87	75	16	38	8	54
34	100	100	59	9	73	84	3	55
35	100	100	87	76	17	27	0	42
41	100	100	100	61	24	56	15	25
CYP# Positive Control c–f					86c	90d	90e	98f

^a% Compound remaining after 60 min as compared to t₀. Final compound concentration is 2 μM.

^b% Inhibition at 10 μM.

^cFurafylline,

^dSulfaphenazole,

^eQuinidine, and

^fKetoconazole were used as positive controls in the CYP450 inhibition assays. The results are from three replicates.