Table 2. Oxazolidinedione Ureas.

						mouse microsomal stability			mouse pharmacokinetics
compd	R1	R2	X	p300 HAT IC50 (μM)	H3K27 Ac IC50 (μM)	CL scaled (L/h/kg)	fu, mica	Clint,u (L/h/kg)	CLp, ivb,f (L/h/kg)	PPB %	CLp,u (L/h/kg)	F % oral	oral AUC (μg·h/mL)
22	Me	cyclopropyl	H	0.025	0.047	107	0.48	188	1.62	99.1	186	40	2.5c
23	CF3	cyclopropyl	F	0.032	0.045	41	0.22	181	0.4	99.8	252	45	1.1d
24	Me	CF3	F	0.060	0.101	21.1	0.56	37.6	0.56	99.2	75	>100	1.94,d11.6e

^aFraction unbound in human microsomes.

^b1 mg/kg dose.

^c10 mg/kg dose.

^d1 mg/kg dose.

^e12.5 mg/kg dose.

^f1L/h/kg = 16.6 mL/min/kg.